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Therapy Name | Tofacitinib |
Synonyms | |
Therapy Description |
Xeljanz (tofacitinib) is a pan-JAK inhibitor, which decreases downstream signaling and potentially leads to reduced tumor cell growth (PMID: 26300391, PMID: 21106989). Xeljanz (tofacitinib) is FDA approved for rheumatoid arthritis (FDA.gov). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Tofacitinib | Xeljanz | Tasocitinib|CP-690550|CP-690,550 | JAK Inhibitor (Pan) - ATP competitive 3 | Xeljanz (tofacitinib) is a pan-JAK inhibitor, which decreases downstream signaling and potentially leads to reduced tumor cell growth (PMID: 26300391, PMID: 21106989). Xeljanz (tofacitinib) is FDA approved for rheumatoid arthritis (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
JAK3 Y100A JAK3 L857P | Advanced Solid Tumor | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib) inhibited Jak3-Stat signaling and cell proliferation in transformed cells over expressing both JAK3 L857P and Y100A in culture (PMID: 26446793). | 26446793 |
JAK3 L875H | hematologic cancer | predicted - sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing JAK3 L875H demonstrated some sensitivity to treatment with Xeljanz (tofacitinib) in culture, but were not as sensitive as cells expressing other JAK3 activating mutations (PMID: 31976485). | 31976485 |
FLT3 exon 14 ins JAK2 V617F | hematologic cancer | resistant | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing a FLT3-ITD mutation and JAK2 V617F were resistant to treatment with Xeljanz (tofacitinib) in culture (PMID: 33149267). | 33149267 |
FLT3 exon 14 ins JAK3 V722I | hematologic cancer | resistant | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing a FLT3-ITD mutation and JAK3 V722I were resistant to treatment with Xeljanz (tofacitinib) in culture (PMID: 33149267). | 33149267 |
JAK3 A572V | Advanced Solid Tumor | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human cells expressing JAK3 A572V in culture demonstrated decreased cell survival, increased G1 arrest, elevated apoptotic activity, and reduced phosphorylation of Stat5a when treated with Xeljanz (tofacitinib) (PMID: 21821710). | 21821710 |
JAK3 V722I | Advanced Solid Tumor | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib) treatment converted cells expressing JAK3 V722I from factor-independent to factor-dependent growth in cell culture (PMID: 25146434). | 25146434 |
JAK3 T1022I | Advanced Solid Tumor | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib) inhibited viability of transformed cells expressing JAK3 T1022I in culture (PMID: 32639993). | 32639993 |
JAK3 L857P | Advanced Solid Tumor | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib) inhibited Jak3-Stat signaling and cell proliferation in transformed cells over expressing JAK3 L857P in culture (PMID: 26446793). | 26446793 |
JAK3 V674A | Advanced Solid Tumor | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib) inhibited Jak3-Stat signaling and cell proliferation in transformed cells over expressing JAK3 V674A in culture (PMID: 26446793). | 26446793 |
CSF3R S783fs | chronic neutrophilic leukemia | predicted - resistant | Tofacitinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, cells derived from a patient with chronic neutrophilic leukemia harboring CSF3R S783fs did not respond to treatment with Xeljanz (tofacitinib) in culture (PMID: 23656643). | 23656643 |
JAK3 H583Y | hematologic cancer | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib) decreased viability of transformed mouse Ba/F3 cells expressing JAK3 H583Y (PMID: 28284718). | 28284718 |
JAK3 A572V | mature T-cell and NK-cell lymphoma | sensitive | Tofacitinib | Preclinical | Actionable | In a preclinical study, Xeljanz (tofacitinib), a pan-JAK inhibitor, reduced cell viability and increased apoptosis in a JAK3 A572V mutant natural killer/T-cell lymphoma cell line (PMID: 22705984). | 22705984 |
JAK3 A573V | hematologic cancer | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib, CP-690,550) decreased cell viability in transformed mouse Ba/F3 cells expressing Jak3 A573V (PMID: 29046866). | 29046866 |
JAK3 L156P | Advanced Solid Tumor | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human cells expressing JAK3 L156P in culture demonstrated decreased cell survival, increased G1 arrest, and reduced phosphorylation of Stat5a when treated with Xeljanz (tofacitinib) (PMID: 21821710). | 21821710 |
JAK3 E183G | Advanced Solid Tumor | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human cells expressing JAK3 E183G in culture demonstrated decreased cell survival, increased G1 arrest, elevated apoptotic activity, and reduced phosphorylation of Stat5a when treated with Xeljanz (tofacitinib) (PMID: 21821710). | 21821710 |
JAK3 R172Q | Advanced Solid Tumor | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human cells expressing JAK3 R172Q in culture demonstrated decreased cell survival, reduced phosphorylation of Stat5a, and G1 arrest when treated with Xeljanz (tofacitinib) (PMID: 21821710). | 21821710 |
JAK3 M511I | hematologic cancer | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib, CP-690,550) decreased cell viability in transformed mouse Ba/F3 cells expressing Jak3 M511I (PMID: 29046866). | 29046866 |
JAK3 M511I | T-cell acute lymphoblastic leukemia | sensitive | Tofacitinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib) treatment inhibited downstream signaling, induced apoptosis, and reduced cell viability of patient-derived T-cell acute lymphoblastic leukemia cell lines harboring JAK3 M511I (PMID: 35411095). | 35411095 |
JAK3 Q988P | hematologic cancer | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib) inhibited growth of transformed cells expressing JAK3 Q988P in culture (PMID: 37712558). | 37712558 |
JAK3 G589D | hematologic cancer | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xeljanz (tofacitinib, CP-690,550) decreased cell viability in transformed mouse Ba/F3 cells expressing Jak3 G589D (PMID: 28284718). | 28284718 |
JAK3 L857Q | hematologic cancer | sensitive | Tofacitinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing JAK3 L857Q were sensitive to treatment with Xeljanz (tofacitinib) in culture, demonstrating decreased cell proliferation (PMID: 31976485). | 31976485 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT05326464 | Phase III | Tofacitinib | Tofacitinib in Recurrent GBM Patients | Recruiting | USA | 0 |