Missing content? – Request curation!
Request curation for specific Genes, Variants, or PubMed publications.
Have questions, comments, or suggestions? - Let us know!
Email us at : ckbsupport@genomenon.com
Therapy Name | Regorafenib |
Synonyms | |
Therapy Description |
Stivarga (regorafenib) is an inhibitor of several kinases including VEGFR, RET, KIT, PDGFR and RAF, thereby inhibiting tumor angiogenesis and tumor cell proliferation (PMID: 24756792). Stivarga (regorafenib) is FDA approved for colorectal cancer, hepatocellular carcinoma, and GIST (FDA.gov). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Regorafenib | Stivarga | BAY 73-4506 | BRAF Inhibitor 25 CRAF Inhibitor 12 KIT Inhibitor 57 PDGFR Inhibitor (Pan) 30 RET Inhibitor 53 VEGFR Inhibitor (Pan) 36 VEGFR2 Inhibitor 37 | Stivarga (regorafenib) is an inhibitor of several kinases including VEGFR, RET, KIT, PDGFR and RAF, thereby inhibiting tumor angiogenesis and tumor cell proliferation (PMID: 24756792). Stivarga (regorafenib) is FDA approved for colorectal cancer, hepatocellular carcinoma, and GIST (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
KIT exon17 | melanoma | sensitive | Regorafenib | Case Reports/Case Series | Actionable | In a Phase II trial, second or later-line Stivarga (regorafenib) treatment resulted in a disease control rate of 73.9% (17/23, 2 complete responses, 5 partial responses), an objective response rate of 30.4% (7/23), and median overall survival (mOS) of 21.5 months in patients with melanoma harboring KIT exon 9, 11, 13, or 17 mutations, and improved mOS in patients with non-exon 11 mutations compared to patients with exon 11 mutations (24.9 mo vs 18.3 mo, P=0.042) (PMID: 37741071; NCT02501551). | 37741071 |
VHL del | renal cell carcinoma | predicted - sensitive | Regorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited angiogenesis and tumor growth in cell line xenograft models of renal cell carcinoma harboring VHL gene deletion (PMID: 21170960). | 21170960 |
KIT exon 11 del KIT D816E | gastrointestinal stromal tumor | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited proliferation of gastrointestinal stromal tumor cells harboring both KIT exon 11 deletion and KIT D816E in culture (PMID: 31085175). | 31085175 |
KIT D816Y | mast cell neoplasm | predicted - resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, mouse mastocytoma cells harboring KIT D814Y (corresponds to D816Y in human) were resistant to Stivarga (regorafenib) in culture (PMID: 31085175). | 31085175 |
KIT K558delinsNP | Advanced Solid Tumor | sensitive | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT K558delinsNP demonstrated sensitivity to treatment with Stivarga (regorafenib) in culture, resulting in reduced cell viability (PMID: 25239608). | 25239608 |
KIT V560G KIT D816V | mast cell neoplasm | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, mast cells harboring both KIT D816V and KIT V560G were resistant to Stivarga (regorafenib) in culture (PMID: 31085175). | 31085175 |
KIT P551_E554del | Advanced Solid Tumor | resistant | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT P551_E554del were resistant to treatment with Stivarga (regorafenib) in culture (PMID: 25239608). | 25239608 |
KIT V560_L576del KIT V654A | gastrointestinal stromal tumor | sensitive | Regorafenib | Preclinical - Pdx | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT V560_L576del and V654A with overexpression of GPR20 (IHC score 3+) (PMID: 33579785). | 33579785 |
KIT W557_K558del KIT T670I | Advanced Solid Tumor | decreased response | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT T670I demonstrated a decreased response to treatment with Stivarga (regorafenib) compared to cells expressing KIT W557_K558del alone in culture (PMID: 25239608). | 25239608 |
KIT W557_K558del KIT T670I | Advanced Solid Tumor | decreased response | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del and KIT T670I demonstrated a decreased response to treatment with Stivarga (regorafenib) compared to cells expressing KIT W557_K558del alone in culture (PMID: 32350132). | 32350132 |
MAP2K1 I111S | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 I111S displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
KIT W557_K558del KIT D820A | Advanced Solid Tumor | conflicting | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del and KIT D820A were sensitive to treatment with Stivarga (regorafenib), demonstrating reduced cell viability in culture (PMID: 32350132). | 32350132 |
KIT W557_K558del KIT D820A | Advanced Solid Tumor | conflicting | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820A were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
BRAF V600E PIK3CA P449T | colorectal cancer | resistant | Regorafenib | Preclinical | Actionable | In a preclinical study, human colorectal cancer cells harboring BRAF V600E and PIK3CA P449T were resistant to Stivarga (regorafenib) in culture (PMID: 25838391). | 25838391 |
BRAF V600E | colorectal cancer | sensitive | Regorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited proliferation of colorectal cancer cells harboring BRAF V600E in culture and suppressed angiogenesis and tumor growth in cell line xenograft models (PMID: 21170960). | 21170960 |
KIT V560_Y578del | gastrointestinal stromal tumor | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited growth of a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del in culture, but was less potent compared to AZD3229 (PMID: 32350132). | 32350132 |
KIT exon9 | melanoma | predicted - sensitive | Regorafenib | Case Reports/Case Series | Actionable | In a Phase II trial, second or later-line Stivarga (regorafenib) treatment resulted in a disease control rate of 73.9% (17/23, 2 complete responses, 5 partial responses), an objective response rate of 30.4% (7/23), and median overall survival (mOS) of 21.5 months in patients with melanoma harboring KIT exon 9, 11, 13, or 17 mutations, and improved mOS in patients with non-exon 11 mutations compared to patients with exon 11 mutations (24.9 mo vs 18.3 mo, P=0.042) (PMID: 37741071; NCT02501551). | 37741071 |
KIT W557_K558del KIT Y823D | gastrointestinal stromal tumor | sensitive | Regorafenib | Preclinical - Pdx | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT W557_K558del and KIT Y823D (PMID: 32350132). | 32350132 |
KIT V560G | mast cell neoplasm | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited proliferation of mast cells harboring KIT V560G in culture (PMID: 31085175). | 31085175 |
KIT K642E KIT N822K | gastrointestinal stromal tumor | sensitive | Regorafenib | Preclinical - Pdx | Actionable | In a preclinical study, Stivarga (regorafenib) suppressed tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT K642E and KIT N822K, but was less potent in comparison to treatment with AZD3229 (PMID: 32350132). | 32350132 |
BRAF mutant | colorectal cancer | no benefit | Regorafenib | Phase II | Actionable | In a Phase II clinical trial (PREVIUM), Stivarga (regorafenib) treatment resulted in 0% (0/15) 6-month progression free survival (PFS), a 2.2-month median PFS, and a median overall survival of 3.3 months in metastatic colorectal cancer patients with KRAS (n=9), NRAS (n=3) or BRAF (n=2) mutations who failed first line therapy; however, the trial was terminated early due to poor accrual (PMID: 30120161; NCT02175654). | 30120161 |
KIT A502_Y503dup KIT V654A | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT A502_Y503dup and KIT V654A demonstrated resistance to Stivarga (regorafenib) in culture (PMID: 32350132). | 32350132 |
MAP2K1 Q56P | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 Q56P displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
KIT T670I | Advanced Solid Tumor | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT T670I demonstrated sensitivity to Stivarga (regorafenib) treatment in culture, resulting in reduced cell viability (PMID: 33212994). | 33212994 |
FGFR1 amp FGFR2 amp | breast cancer | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a breast cancer cell line with FGFR1 and FGFR2 amplification was sensitive to treatment with Stivarga (regorafenib), demonstrating inhibition of cell growth in culture (PMID: 33563752). | 33563752 |
KIT exon11 | gastrointestinal stromal tumor | sensitive | Regorafenib | Phase II | Actionable | In a Phase II clinical trial, treatment with Stivarga (regorafenib) resulted in a clinical benefit rate of 76% (25/33), a median progression-free survival (PFS) of 13.2 months, and a median overall survival of 25 months in patients with gastrointestinal stromal tumors, with patients with KIT exon 11 mutations demonstrating the longest PFS of 13.4 months (PMID: 27371698). | 27371698 |
KIT exon11 | gastrointestinal stromal tumor | sensitive | Regorafenib | Guideline | Actionable | Stivarga (regorafenib) is included in guidelines as third-line or subsequent therapy for locally advanced, unresectable, or metastatic gastrointestinal stromal tumor (GIST) patients harboring sensitizing mutations, such as KIT exon 11 mutations (PMID: 34560242; ESMO.org). | 34560242 detail... |
KIT exon13 | melanoma | sensitive | Regorafenib | Case Reports/Case Series | Actionable | In a Phase II trial, second or later-line Stivarga (regorafenib) treatment resulted in a disease control rate of 73.9% (17/23, 2 complete responses, 5 partial responses), an objective response rate of 30.4% (7/23), and median overall survival (mOS) of 21.5 months in patients with melanoma harboring KIT exon 9, 11, 13, or 17 mutations, and improved mOS in patients with non-exon 11 mutations compared to patients with exon 11 mutations (24.9 mo vs 18.3 mo, P=0.042) (PMID: 37741071; NCT02501551). | 37741071 |
KIT exon9 | Advanced Solid Tumor | resistant | Regorafenib | Preclinical | Actionable | In a preclinical study, Stivarga (regorafineb) had no effect on transformed cells expressing a KIT exon 9 mutation in culture (PMID: 25239608). | 25239608 |
KIT N655K | Advanced Solid Tumor | decreased response | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT N655K demonstrated a reduced response to Stivarga (regorafenib) treatment compared to cells expressing KIT T670I in culture (PMID: 33212994). | 33212994 |
FGFR3 fusion | urinary bladder cancer | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, bladder cancer cell lines harboring an FGFR3 fusion were sensitive to treatment with Stivarga (regorafenib), demonstrating inhibition of cell growth (PMID: 33563752). | 33563752 |
KIT W557_K558del KIT D816G | Advanced Solid Tumor | resistant | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816G were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
KIT exon11 | melanoma | sensitive | Regorafenib | Phase II | Actionable | In a Phase II trial, second or later-line Stivarga (regorafenib) treatment resulted in a disease control rate of 73.9% (17/23, 2 complete responses, 5 partial responses), an objective response rate of 30.4% (7/23), and median overall survival (mOS) of 21.5 months in patients with melanoma harboring KIT exon 9, 11, 13, or 17 mutations, and improved mOS in patients with non-exon 11 mutations compared to patients with exon 11 mutations (24.9 mo vs 18.3 mo, P=0.042) (PMID: 37741071; NCT02501551). | 37741071 |
KIT act mut | melanoma | predicted - sensitive | Regorafenib | Case Reports/Case Series | Actionable | In a clinical case study, Stivarga (regorafenib) treatment demonstrated safety and preliminary activity in patients with melanoma harboring activating mutations in KIT, resulting in an overall response rate of 100% (7/7, 1 complete and 6 partial responses), with median duration of response and median progression-free survival not reached and response ongoing in 4 patients at a median follow-up of 43 weeks (Ann Oncol (2024) 35 (suppl_2): S743-S744). | detail... |
KIT W557_K558del KIT Y823D | Advanced Solid Tumor | predicted - sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del and KIT Y823D demonstrated sensitivity to treatment with Stivarga (regorafenib), but was decreased compared to cells expressing KIT W557_K558del alone in culture (PMID: 32350132). | 32350132 |
RET C634W | thyroid cancer | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited proliferation of thyroid cancer cells harboring RET C634W in culture (PMID: 21170960). | 21170960 |
KIT V560_Y578del KIT V654A | gastrointestinal stromal tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del and KIT V654A demonstrated resistance to Stivarga (regorafenib) in culture (PMID: 32350132). | 32350132 |
KIT exon11 KIT T670I | gastrointestinal stromal tumor | predicted - sensitive | Regorafenib | Preclinical - Pdx | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited Kit signaling, resulted in tumor growth inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT exon 11 mutation (K550_splice) and KIT T670I, which was established from a patient who did not respond to Gleevec (imatinib mesylate) (PMID: 29100343). | 29100343 |
KIT exon 11 del | gastrointestinal stromal tumor | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited Kit phosphorylation and proliferation of gastrointestinal stromal tumor cells harboring KIT exon 11 deletion in culture (PMID: 31085175). | 31085175 |
FGFR2 amp FGFR2 over exp | stomach cancer | no benefit | Regorafenib | Case Reports/Case Series | Actionable | In a Phase II trial, gastric cancer patients (n=3/35) with FGFR2 amplification and FGFR2 overexpression did not achieve an objective response when treated with Stivarga (regorafenib) (PMID: 33563752). | 33563752 |
KIT D816V | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT D816V were resistant to Stivarga (regorafenib) in culture (PMID: 31085175). | 31085175 |
KIT W557_K558del KIT N822K | Advanced Solid Tumor | conflicting | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del and KIT N822K was sensitive to treatment with Stivarga (regorafenib), demonstrating decreased cell viability in culture (PMID: 32350132). | 32350132 |
KIT W557_K558del KIT N822K | Advanced Solid Tumor | conflicting | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT N822K were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
MAP2K1 K57N | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 K57N displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
KIT D816H | Advanced Solid Tumor | resistant | Regorafenib | Preclinical | Actionable | In a preclinical study, KIT D816H demonstrated resistance to Stivarga (regorafenib) in an in vitro assay, and conferred secondary resistance to Stivarga (regorafenib) in transformed cells expressing other KIT mutations (PMID: 25239608). | 25239608 |
KIT V560D KIT D820A | Advanced Solid Tumor | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) treatment resulted in decreased viability of transformed cells expressing KIT V560D and KIT D820A in culture, but was less effective compared to other treatments (PMID: 32350132). | 32350132 |
KIT V560D KIT D816H | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT V560D and KIT D816H demonstrated resistance to Stivarga (regorafenib) in culture (PMID: 32350132). | 32350132 |
FGFR1 over exp | stomach cancer | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Stivarga (regorafenib) in an FGFR1-overexpressing gastric cancer cell line resulted in decreased phosphorylation of Fgfr2 and Erk, and inhibition of cell growth in culture (PMID: 33563752). | 33563752 |
MAP2K1 V211D | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 V211D displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
KIT P551_K558del | Advanced Solid Tumor | sensitive | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT P551_K558del (reported as K550_W557del) demonstrated sensitivity to treatment with Stivarga (regorafenib) in culture, resulting in reduced cell viability (PMID: 25239608). | 25239608 |
KIT A502_Y503dup KIT D816H | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT A502_Y503dup and KIT D816H demonstrated resistance to Stivarga (regorafenib) in culture (PMID: 32350132). | 32350132 |
FGFR2 amp | colorectal cancer | predicted - sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited Fgfr2 signaling and proliferation of FGFR2-amplified colorectal cancer cells in culture (PMID: 29573334). | 29573334 |
FGFR2 amp | colorectal cancer | predicted - sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, a colorectal cancer cell line with FGFR1 and FGFR2 amplification was sensitive to treatment with Stivarga (regorafenib), demonstrating inhibition of cell growth in culture (PMID: 33563752). | 33563752 |
KIT W557_K558del KIT A829P | Advanced Solid Tumor | conflicting | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT A829P were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
KIT W557_K558del KIT A829P | Advanced Solid Tumor | conflicting | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del and KIT A829P were sensitive to treatment with Stivarga (regorafenib), but demonstrated a decreased response compared to cells expressing KIT W557_K558del alone in culture (PMID: 32350132). | 32350132 |
KIT A502_Y503dup | Advanced Solid Tumor | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) treatment resulted in decreased viability of transformed cells expressing KIT A502_Y503dup in culture, but was less potent compared to treatment with AZD3229 (PMID: 32350132). | 32350132 |
KIT W557_K558del KIT D816H | Advanced Solid Tumor | decreased response | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D816H demonstrated a decreased response to treatment with Stivarga (regorafenib) in culture (PMID: 25239608). | 25239608 |
KIT V560D KIT V654A | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing KIT V560D and KIT V654A demonstrated resistance to treatment with Stivarga (regorafenib) in culture (PMID: 32350132). | 32350132 |
KIT Y570_L576del KIT D816E PTEN T321fs | gastrointestinal stromal tumor | sensitive | Regorafenib | Preclinical - Pdx | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited Kit, Erk, and Mtor signaling, resulted in tumor growth inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT D816E, KIT Y570_L576del, and PTEN T321fs, which was established from a patient who did not respond to Gleevec (imatinib mesylate), Sutent (sunitinib), and Nexavar (sorafenib) (PMID: 29100343). | 29100343 |
NRAS mutant | colorectal cancer | no benefit | Regorafenib | Phase II | Actionable | In a Phase II clinical trial (PREVIUM), Stivarga (regorafenib) treatment resulted in 0% (0/15) 6-month progression free survival (PFS), a 2.2-month median PFS, and a median overall survival of 3.3 months in metastatic colorectal cancer patients with KRAS (n=9), NRAS (n=3) or BRAF (n=2) mutations who failed first line therapy; however, the trial was terminated early due to poor accrual (PMID: 30120161; NCT02175654). | 30120161 |
KIT N822K | acute myeloid leukemia | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited proliferation of acute myeloid leukemia cells harboring KIT N822K in culture (PMID: 31085175). | 31085175 |
KIT K642E | gastrointestinal stromal tumor | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited proliferation of gastrointestinal stromal tumor cells harboring KIT K642E in culture (PMID: 21170960). | 21170960 |
FGFR2 amp | stomach cancer | sensitive | Regorafenib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited Fgfr2 signaling and proliferation of FGFR2-amplified gastric cancer cell lines in culture, resulted in tumor growth inhibition in cell line xenograft models (PMID: 29573334). | 29573334 |
FGFR2 amp | stomach cancer | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, treatment with Stivarga (regorafenib) in gastric cancer cell lines harboring FGFR2 amplification resulted in decreased phosphorylation of Fgfr2 and Erk, and inhibition of cell growth in culture (PMID: 33563752). | 33563752 |
FBXW7 R505C | colorectal cancer | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, colorectal cell lines with FBXW7 R505C demonstrated acquired resistance in regorafenib (PMID: 27399335). | 27399335 |
KIT V560D | Advanced Solid Tumor | sensitive | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT V560D demonstrated sensitivity to treatment with Stivarga (regorafineb) in culture, resulting in reduced cell viability (PMID: 25239608). | 25239608 |
KIT W557_K558del KIT V654A | Advanced Solid Tumor | resistant | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT V654A demonstrated resistance to treatment with Stivarga (regorafenib) in culture (PMID: 25239608). | 25239608 |
KIT A502_Y503dup | gastrointestinal stromal tumor | predicted - sensitive | Regorafenib | Preclinical - Pdx | Actionable | In a preclinical study, Stivarga (regorafenib) did not significantly inhibit Kit, Erk, or Mtor signaling, but resulted in tumor growth inhibition in patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT A502_Y503dup and KIT D820E, which was established from a patient who did not respond to Gleevec (imatinib mesylate) and Sutent (sunitinib) (PMID: 29100343). | 29100343 |
MAP2K1 F129L | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 F129L displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
KIT exon 11 del KIT T670I | gastrointestinal stromal tumor | sensitive | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Stivarga (regorafenib) inhibited proliferation of gastrointestinal stromal tumor cells harboring both KIT exon 11 deletion and KIT T670I in culture (PMID: 31085175). | 31085175 |
MAP2K1 F53L | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 F53L displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
KIT exon9 | gastrointestinal stromal tumor | sensitive | Regorafenib | Guideline | Actionable | Stivarga (regorafenib) is included in guidelines as third-line or subsequent therapy for locally advanced, unresectable, or metastatic gastrointestinal stromal tumor (GIST) patients harboring sensitizing mutations, such as KIT exon 9 mutations (PMID: 34560242; ESMO.org). | 34560242 detail... |
KIT W557_K558del KIT D820G | Advanced Solid Tumor | resistant | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells co-expressing KIT W557_K558del and KIT D820G were resistant to Stivarga (regorafenib) in an in vitro kinase assay (PMID: 25239608). | 25239608 |
MAP2K1 C121S | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 C121S displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
KIT W557_K558del | Advanced Solid Tumor | sensitive | Regorafenib | Preclinical | Actionable | In a preclinical study, transformed cells expressing KIT W557_K558del demonstrated sensitivity to treatment with Stivarga (regorafineb) in culture, resulting in reduced cell viability (PMID: 25239608). | 25239608 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT01896856 | Phase Ib/II | Guadecitabine + Irinotecan Regorafenib | Phase I Study of SGI-110 With Irinotecan Followed by Randomized Phase II Study of SGI-110 With Irinotecan Versus Regorafenib in Previously Treated Metastatic Colorectal Cancer | Completed | USA | NLD | 0 |
NCT06087263 | Phase II | Regorafenib | Phase 2 Study to Evaluate the Efficacy of Regorafenib in Specific GIST Mutation Subsets (KIT Exon 17, 18, or 14 Mutation and SDHB Deficient GIST) in the Post-imatinib Second-line Setting. | Recruiting | USA | 0 |
NCT01538680 | Phase III | Regorafenib | Regorafenib in Subjects With Metastatic Colorectal Cancer (CRC) Who Have Progressed After Standard Therapy | No longer available | USA | SWE | POL | NOR | NLD | ITA | ISR | IRL | HUN | GRC | GBR | FRA | FIN | ESP | DNK | DEU | CZE | CHE | CAN | BEL | AUT | AUS | 3 |
NCT02693535 | Phase II | Cobimetinib + Vemurafenib Atezolizumab + Talazoparib Regorafenib Larotrectinib Trastuzumab + Tucatinib Ipilimumab + Nivolumab Palbociclib Afatinib Entrectinib Talazoparib Pembrolizumab Temsirolimus Pertuzumab + Trastuzumab Atezolizumab + Pertuzumab/trastuzumab/hyaluronidase-zzxf Crizotinib Abemaciclib Sunitinib Olaparib | TAPUR: Testing the Use of Food and Drug Administration (FDA) Approved Drugs That Target a Specific Abnormality in a Tumor Gene in People With Advanced Stage Cancer (TAPUR) | Recruiting | USA | 0 |
NCT04051606 | Phase II | Regorafenib | Phase II Study of Regorafenib in Bevacizumab Refractory Recurrent Glioblastoma | Active, not recruiting | USA | 0 |
NCT05425940 | Phase III | Atezolizumab + XL092 Regorafenib | Study of XL092 + Atezolizumab vs Regorafenib in Subjects With Metastatic Colorectal Cancer (STELLAR-303) | Active, not recruiting | USA | POL | NZL | HUN | GBR | FRA | ESP | DEU | BEL | AUS | 6 |
NCT02581059 | Phase II | Regorafenib | Efficacy of Ginseng for Patients on Regorafenib | Terminated | USA | 0 |
NCT05370807 | Phase II | Regorafenib | A Clinical Trial of Regorafenib in Patients With Pretreated Advanced Melanoma (RegoMel) | Recruiting | BEL | 0 |
NCT02234180 | Phase II | Regorafenib | Study of Adjuvant Regorafenib vs Placebo in Patients With Node Positive Esophageal Cancer That Completed Pre-operative Therapy | Terminated | USA | 0 |
NCT02316340 | Phase II | Vorinostat Hydroxychloroquine Regorafenib | Vorinostat Plus Hydroxychloroquine Versus Regorafenib in Colorectal Cancer | Completed | USA | 0 |
NCT02053376 | Phase II | Regorafenib | A Phase 2 Trial of Regorafenib as A Single Agent in Advanced and Metastatic Biliary Tract Carcinoma/Cholangiocarcinoma Patients Who Have Failed First-line Chemotherapy | Completed | USA | 0 |
NCT01939223 | Phase III | Regorafenib | COlorectal Cancer Treated With Adjuvant Regorafenib Versus Placebo After Curative Treatment of Liver Metastases in a Randomized, Double-blind, Placebo?Controlled Phase-III STudy (COAST) | Terminated | USA | ITA | ISR | GBR | FRA | ESP | DEU | CAN | BRA | BEL | AUS | 3 |
NCT06275919 | Phase II | Regorafenib | Regorafenib for Recurrent Grade 2 and 3 Meningioma (MIRAGE Trial) (MIRAGE) | Recruiting | ITA | 0 |
NCT01103323 | Phase III | Regorafenib | Patients With Metastatic Colorectal Cancer Treated With Regorafenib or Placebo After Failure of Standard Therapy | Completed | USA | TUR | NLD | ITA | ISR | HUN | FRA | ESP | DEU | CHE | CAN | BRA | BEL | AUS | ARG | 4 |
NCT02795156 | Phase II | Cabozantinib Afatinib Regorafenib | Study Assessing Activity of Molecularly Matched Targeted Therapies in Select Tumor Types Based on Genomic Alterations | Completed | USA | 0 |
NCT04117945 | Phase II | Regorafenib Irinotecan + Panitumumab Panitumumab Cetuximab + Irinotecan Cetuximab | Regorafenib, With Cetuximab or Panitumumab, for the Treatment of Unresectable, Locally Advanced, or Metastatic Colorectal Cancer | Active, not recruiting | USA | 0 |
NCT02098538 | Phase II | Regorafenib | Regorafenib in Patients With Progressive, Recurrent/Metastatic Adenoid Cystic Carcinoma | Completed | USA | 0 |
NCT02638766 | Phase II | Regorafenib | Single Agent Regorafenib in First-line for Metastatic/Unresectable KIT/PDGFR Wild Type GIST (REGISTRI) | Completed | ITA | FRA | ESP | 0 |
NCT02023333 | Phase II | Regorafenib | Regorafenib in Good Performance Status Patients With Newly Diagnosed Metastatic Colorectal Adenocarcinoma | Active, not recruiting | USA | 0 |
NCT03377361 | Phase Ib/II | Regorafenib Ipilimumab + Nivolumab + Trametinib Nivolumab + Trametinib | An Investigational Immuno-therapy Study Of Nivolumab In Combination With Trametinib With Or Without Ipilimumab In Participants With Previously Treated Cancer of the Colon or Rectum That Has Spread (CheckMate 9N9) | Active, not recruiting | USA | ITA | ESP | DEU | CZE | CAN | BEL | AUS | ARG | 1 |
NCT05395741 | Phase Ib/II | Regorafenib | Regorafenib in Patients With Refractory Primary Bone Tumors (Regbone) | Recruiting | POL | 0 |
NCT02466009 | Phase II | Regorafenib | Regorafenib in Metastatic Colorectal Cancer | Completed | USA | 0 |
NCT03970447 | Phase II | Lomustine Regorafenib Temozolomide | A Trial to Evaluate Multiple Regimens in Newly Diagnosed and Recurrent Glioblastoma (GBM AGILE) | Recruiting | USA | FRA | DEU | CHE | CAN | AUS | 0 |
NCT03563157 | Phase Ib/II | Aldoxorubicin + Avelumab + Capecitabine + Cetuximab + Cyclophosphamide + ETBX-011 + ETBX-021 + ETBX-051 + ETBX-061 + Fluorouracil + GI-4000 + GI-6207 + GI-6301 + haNK cells + Leucovorin + Nab-paclitaxel + Nogapendekin alfa inbakicept + Oxaliplatin + Regorafenib + Trastuzumab Regorafenib | QUILT 3.071: NANT Colorectal Cancer (CRC) Vaccine | Active, not recruiting | USA | 0 |
NCT05159245 | Phase II | Vemurafenib Tepotinib Vismodegib Apalutamide Alectinib Regorafenib Entrectinib Pertuzumab + Trastuzumab Pemigatinib Atezolizumab Cobimetinib Dabrafenib + Trametinib Dabrafenib Trametinib Abemaciclib | The Finnish National Study to Facilitate Patient Access to Targeted Anti-cancer Drugs (FINPROVE) | Recruiting | FIN | 0 |
NCT03844620 | Phase II | Regorafenib Trifluridine-tipiracil hydrochloride Regorafenib + Trifluridine-tipiracil hydrochloride | Circulating Cell-Free Tumor DNA Testing in Guiding Treatment for Patients With Advanced or Metastatic Colorectal Cancer | Active, not recruiting | USA | 0 |
NCT02080260 | Phase II | Regorafenib | A Study of Regorafenib in Advanced Pancreatic Cancer Patients | Completed | USA | 0 |
NCT02439723 | Phase I | Regorafenib | Effects of LBM and PPIs on Pharmacokinetics and Safety of Regorafenib (BAY 73-4506) in Cancer Patients | Withdrawn | CAN | 0 |
NCT02459119 | Phase II | Regorafenib | Study of Regorafenib for Urothelial Cancer Following Chemotherapy (UAB 1477) | Completed | USA | 0 |
NCT02096354 | Phase II | Regorafenib | A Phase 2 Randomized, Open-Label Study of RRx-001 vs Regorafenib in Subjects With Metastatic Colorectal Cancer | Completed | USA | 0 |
NCT02287727 | Phase II | Regorafenib | Regorafenib in Reducing Recurrence in Patients With Non-metastatic Rectal Cancer Who Have Completed Curative-Intent Treatment | Withdrawn | USA | 0 |
NCT02788279 | Phase III | Atezolizumab Atezolizumab + Cobimetinib Regorafenib | A Study to Investigate Efficacy and Safety of Cobimetinib Plus Atezolizumab and Atezolizumab Monotherapy Versus Regorafenib in Participants With Metastatic Colorectal Adenocarcinoma | Completed | USA | POL | ITA | GBR | ESP | CAN | BEL | AUS | 3 |
NCT03042689 | Phase I | Regorafenib | Study of Regorafenib in Patients With Advanced Myeloid Malignancies | Completed | USA | 0 |
NCT02259725 | Phase II | Regorafenib | Regorafenib in Treating Patients With Advanced or Metastatic Neuroendocrine Tumors | Completed | USA | 0 |
NCT02587650 | Phase II | Ceritinib Capmatinib Regorafenib Entrectinib | Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma | Terminated | USA | 0 |
NCT01853046 | Phase I | Regorafenib | Pharmacokinetics and Safety of Regorafenib (BAY73-4506) in Cancer Subjects With Severe Renal Impairment | Completed | USA | CAN | 0 |
NCT05366816 | Phase II | Regorafenib Sunitinib | ctDNA-Guided Sunitinib And Regorafenib Therapy for GIST | Recruiting | USA | 0 |
NCT04476329 | Phase II | Regorafenib | Optimization for Regorafenib in HCC (ReDos HCC) | Terminated | USA | 0 |
NCT04055220 | FDA approved | Regorafenib | Efficacy and Safety of Regorafenib as Maintenance Therapy After First-line Treatment in Patients With Bone Sarcomas (REGOSTA) | Recruiting | FRA | 0 |
NCT02119676 | Phase II | Regorafenib Ruxolitinib | Study of Ruxolitinib in Colorectal Cancer Patients | Terminated | USA | ISR | GBR | FRA | ESP | DEU | AUS | 1 |
NCT02402036 | Phase II | Regorafenib | A Biomarker Study in Patients Getting Regorafenib for Metastatic Colorectal Cancer | Terminated | USA | 0 |
NCT02278783 | Phase II | Regorafenib | Phase 2 Trial of Regorafenib in Patients With Recurrent Ovarian, Primary Peritoneal and Fallopian Tube Cancer | Terminated | USA | 0 |
NCT02466802 | Phase I | Regorafenib Sildenafil | Study of Regorafenib and Sildenafil for Advanced Solid Tumors | Completed | USA | 0 |
NCT01949194 | Phase II | Regorafenib | Study to Determine the Efficacy of Regorafenib in Metastatic Colorectal Cancer Patients and to Discover Biomarkers | Unknown status | CAN | 0 |
NCT03793361 | Phase II | Regorafenib | Phase II Study of Regorafenib as Maintenance Therapy | Active, not recruiting | FRA | 0 |
NCT02241720 | Phase II | Regorafenib | Regorafenib Second Line Treatment of Metastatic or Advanced Upper GI Cancers | Terminated | USA | 0 |
NCT04327700 | Phase II | Regorafenib | Study Of Intrabucally Administered Electromagnetic Fields and Regorafenib | Terminated | USA | 0 |
NCT06246643 | Phase II | Regorafenib | A Study of Continued Treatment With Regorafenib in Participants With Solid Tumors Who Have Participated in Other Bayer Studies | Active, not recruiting | FRA | ESP | 3 |
NCT02048371 | Phase II | Regorafenib | A Blanket Protocol to Study Oral Regorafenib in Patients With Refractory Liposarcoma, Osteogenic Sarcoma, and Ewing/Ewing-like Sarcomas | Completed | USA | 0 |
NCT02425683 | Phase II | Regorafenib | Study of Colorectal Cancer Patients (Stage IIIC) With Either Regorafenib or Standard of Care (No Treatment) After Adjuvant FOLFOX | Terminated | USA | 0 |
NCT02389244 | Phase II | Regorafenib | A Phase II Study Evaluating Efficacy and Safety of Regorafenib in Patients With Metastatic Bone Sarcomas (REGOBONE) | Recruiting | FRA | 0 |
NCT02287025 | FDA approved | Regorafenib | A Phase 4 Study of Regorafenib in Metastatic Colorectal Cancer - Does Educating Physicians Change Patient Out Comes? | Terminated | USA | 0 |
NCT04787341 | Phase II | Regorafenib Panitumumab | PAnitumumab REchallenge Followed by REgorafenib Versus the Reverse Sequence (PARERE) | Recruiting | ITA | 0 |
NCT02048722 | Phase II | Regorafenib | Daily Oral Regorafenib for Chemotherapy-Refractory, Metastatic and Locally Advanced Angiosarcoma | Completed | USA | 0 |
NCT03627728 | Phase II | Regorafenib | Study Maintenance Regorafenib vs Placebo, no Progression Patients After I Line Chemotherapy Metastatic Gastric Cancer (a-MANTRA) | Unknown status | ITA | 0 |
NCT02773524 | Phase III | Regorafenib | A Study of Regorafenib in Refractory Advanced Gastro-Oesophageal Cancer (INTEGRATEII) | Unknown status | USA | NZL | CAN | AUS | 3 |
NCT02934529 | Phase III | Cetuximab + Fluorouracil + Irinotecan + Leucovorin Bevacizumab + Capecitabine + Fluorouracil + Leucovorin Regorafenib | Metastatic Colorectal Cancer (RAS-wildtype) After Response to First-line Treatment With FOLFIR Plus Cetuximab (AIO-KRK-0114) | Active, not recruiting | DEU | 0 |
NCT05622136 | Phase II | Regorafenib | Dose-escalation of Regorafenib in Advanced Hepatocellular Carcinoma (STRAT-aHCC) | Recruiting | BRA | 0 |
NCT02657551 | Phase II | Regorafenib | A Study Using Regorafenib as Second or Third Line Therapy in Metastatic Medullary Thyroid Cancer | Active, not recruiting | USA | 0 |
NCT04776148 | Phase III | Regorafenib Trifluridine-tipiracil hydrochloride Lenvatinib + Pembrolizumab | Study of Lenvatinib (MK-7902/E7080) in Combination With Pembrolizumab (MK-3475) Versus Standard of Care in Participants With Metastatic Colorectal Cancer (MK-7902-017/E7080-G000-325/LEAP-017) | Completed | USA | TUR | ISR | GBR | ESP | DNK | DEU | CAN | AUS | ARG | 5 |
NCT02195011 | Phase II | Regorafenib | Safety Study of Regorafenib and SIR-Spheres® Microspheres Radioembolization in Patients With Refractory Metastatic Colorectal Cancer With Liver Metastases | Completed | USA | 0 |
NCT02115542 | Phase II | Regorafenib | Single Agent Regorafenib in Refractory Advanced Biliary Cancers | Completed | USA | 0 |
NCT03465722 | Phase III | Regorafenib Avapritinib | (VOYAGER) Study of Avapritinib vs Regorafenib in Patients With Locally Advanced Unresectable or Metastatic GIST | Completed | USA | SWE | POL | NLD | ITA | HUN | GBR | FRA | ESP | DEU | CZE | CAN | BEL | AUT | AUS | 3 |
NCT03829462 | Phase III | Regorafenib Irinotecan + Regorafenib | Assessing a Regorafenib-irinotecan Combination Versus Regorafenib Alone in Metastatic Colorectal Cancer Patients (NEXT-REGIRI) | Active, not recruiting | FRA | 0 |
NCT04874207 | FDA approved | Regorafenib | Evaluation of Treatment PERSOnalization Based on Its Therapeutic Monitoring in Patients With Metastatic Colorectal Cancer Treated With REgorafenib (RePERSO) | Active, not recruiting | FRA | 0 |
NCT04698785 | Phase II | Regorafenib | Efficacy of Regorafenib Combined With Best Supportive Care as Maintenance Treatment in High Grade Bone Sarcomas Patients (REGOMAIN) | Recruiting | FRA | 0 |
NCT03992456 | Phase II | Panitumumab Regorafenib Trifluridine-tipiracil hydrochloride | Panitumumab, Regorafenib, or TAS-102, in Treating Patients With Metastatic and/or Unresectable RAS Wild-Type Colorectal Cancer | Active, not recruiting | USA | 0 |
NCT04660812 | Phase Ib/II | AB680 + Etrumadenant + Zimberelimab Regorafenib Bevacizumab + Etrumadenant + Fluorouracil + Leucovorin + Oxaliplatin + Zimberelimab Etrumadenant + Fluorouracil + Leucovorin + Oxaliplatin + Zimberelimab Bevacizumab + Fluorouracil + Leucovorin + Oxaliplatin | An Open Label Study Evaluating the Efficacy and Safety of AB928 Based Treatment Combinations in Patients With Metastatic Colorectal Cancer. | Active, not recruiting | USA | ITA | GBR | FRA | ESP | 1 |
NCT02164240 | Phase I | Sunitinib Regorafenib | Phase Ib Study of SUnitinib Alternating With REgorafenib in Patients With Metastatic and/or Unresectable GIST | Completed | USA | 0 |
NCT01774344 | Phase III | Regorafenib | Study of Regorafenib After Sorafenib in Patients With Hepatocellular Carcinoma (RESORCE) | Completed | USA | NLD | ITA | HUN | GBR | FRA | ESP | DEU | CZE | CHE | BRA | BEL | AUT | AUS | ARG | 6 |
NCT01298570 | Phase II | Fluorouracil + Irinotecan + Leucovorin Regorafenib | Regorafenib+FOLFIRI Versus Placebo+FOLFIRI as 2nd Line Tx in Metastatic Colorectal Cancer | Completed | USA | IRL | 0 |
NCT02664077 | Phase III | Regorafenib | A Study Evaluating Regorafenib Following Completion of Standard Chemotherapy for Patients With Colon Cancer (ARGO) | Terminated | USA | 0 |
NCT02551718 | Phase I | Bosutinib Irinotecan Romidepsin Busulfan Melphalan Nilotinib Crizotinib Cytarabine Mitoxantrone Dasatinib Pazopanib Paclitaxel Clofarabine Hydroxyurea Tretinoin Carfilzomib Nelarabine Bexarotene Pentostatin Everolimus Cabozantinib Mercaptopurine Methotrexate Cladribine Thioguanine Daunorubicin Ponatinib Etoposide Afatinib Gefitinib Gemcitabine Regorafenib Arsenic trioxide Trametinib Imatinib Erlotinib Dabrafenib Decitabine Axitinib Azacitidine Ruxolitinib Fludarabine Lapatinib Ceritinib Sirolimus Sorafenib Lomustine Sunitinib Cabazitaxel Temsirolimus Topotecan Bortezomib Pralatrexate | High Throughput Drug Sensitivity Assay and Genomics- Guided Treatment of Patients With Relapsed or Refractory Acute Leukemia | Completed | USA | 0 |
NCT06425133 | Phase II | Regorafenib Aspirin + Capecitabine + Cyclophosphamide + Regorafenib | Regorafenib in Combination With Multimodal Metronomic Chemotherapy for Chemo-resistant Metastatic Colorectal Cancers (CARE) | Not yet recruiting | FRA | 0 |