Therapy Detail

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Therapy Name	RXDX-105
Synonyms
Therapy Description	Agerafenib (RXDX-105) inhibits wild-type BRAF, BRAF V600E, c-RAF, ABL1 (and BCR-ABL), c-KIT, RET, PDGFR beta, and VEGFR2, potentially resulting in decreased tumor growth (PMID: 22319199, PMID: 31695841).

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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
RXDX-105		AC013773\|CEP-32496\|Agerafenib	ABL Inhibitor (pan) 9 ABL1 Inhibitor 8 BCR-ABL Inhibitor 32 BRAF Inhibitor 26 CRAF Inhibitor 12 KIT Inhibitor 57 PDGFR-beta Inhibitor 14 RET Inhibitor 53 VEGFR2 Inhibitor 37	Agerafenib (RXDX-105) inhibits wild-type BRAF, BRAF V600E, c-RAF, ABL1 (and BCR-ABL), c-KIT, RET, PDGFR beta, and VEGFR2, potentially resulting in decreased tumor growth (PMID: 22319199, PMID: 31695841).

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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
RET rearrange	lung non-small cell carcinoma	predicted - sensitive	RXDX-105	Phase I	Actionable	In a Phase Ib trial, treatment with RXDX-105 (CEP-32496) resulted in an overall response rate of 19% (6/31) and stable disease in 39% (12/31) of patients with treatment-naive non-small cell lung cancer harboring a RET fusion (PMID: 30487236; NCT01877811)	30487236
RET rearrange	lung non-small cell carcinoma	predicted - sensitive	RXDX-105	Case Reports/Case Series	Actionable	In a clinical case study, a patient with non-small cell lung cancer harboring a RET rearrangement demonstrated a sustained partial response following treatment with RXDX-105 (CEP-32496) on a Phase Ib clinical trial (PMID: 28011461; NCT01877811).	28011461
RET rearrange	Advanced Solid Tumor	sensitive	RXDX-105	Preclinical - Pdx	Actionable	In a preclinical study, CEP-32496 (RXDX-105) induced tumor regression in patient-derived xenograft models of several advanced solid tumor type with RET rearrangements (2015 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; Abstract A174).	detail...
BRAF V600E	colon carcinoma	sensitive	RXDX-105	Preclinical - Cell line xenograft	Actionable	In preclinical studies, CEP-32496 (RXDX-105) reduced tumor volume and promoted tumor regression in xenograft models of a BRAF V600E mutant human colon carcinoma cell line (PMID: 22319199).	22319199
BRAF V600E	melanoma	sensitive	RXDX-105	Preclinical - Cell line xenograft	Actionable	In preclinical studies, CEP-32496 (RXDX-105) reduced tumor volume and promoted tumor regression in xenograft models of a BRAF V600E mutant human melanoma cell line (PMID: 22319199).	22319199
EML4 - RET	lung adenocarcinoma	sensitive	RXDX-105	Preclinical - Patient cell culture	Actionable	In a preclinical study, a patient-derived lung adenocarcinoma cell line harboring EML4-RET was sensitive to treatment with Agerafenib (RXDX-105) in culture, demonstrating decreased Akt phosphorylation and induction of apoptosis (PMID: 33795352).	33795352
RET C634W	medullary thyroid carcinoma	sensitive	RXDX-105	Preclinical - Cell culture	Actionable	In a preclinical study, RXDX-105 (CEP-32496) reduced phosphorylation of RET and downstream signaling and inhibited proliferation of a medullary thyroid cancer cell line harboring RET C634W in culture (PMID: 28011461).	28011461

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Clinical Trial	Phase	Therapies	Title	Recruitment Status	Covered Countries	Other Countries
NCT01877811	Phase Ib/II	RXDX-105	CEP-32496 in Patients With Advanced Solid Tumors in Phase 1 and Advanced Melanoma and Metastatic Colorectal Cancer in Phase 2	Completed	USA	0
NCT03784378	Phase I	RXDX-105	Continued Access to RXDX-105	Completed	USA	0
NCT03052569	Expanded access	RXDX-105	Expanded Access to RXDX-105 for Cancers With RET Alterations	No longer available	USA	0

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