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Therapy Name | Selitrectinib |
Synonyms | |
Therapy Description |
Selitrectinib (LOXO-195) is an inhibitor of NTRK1, NTRK2, and NTRK3, which may result in inhibition of tumor growth and tumor regression (PMID: 28578312). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
Selitrectinib | LOXO-195|BAY 2731954 | Trk Receptor Inhibitor (Pan) 31 | Selitrectinib (LOXO-195) is an inhibitor of NTRK1, NTRK2, and NTRK3, which may result in inhibition of tumor growth and tumor regression (PMID: 28578312). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
NTRK1 act mut | Advanced Solid Tumor | predicted - sensitive | Selitrectinib | Preclinical | Actionable | In a preclinical study, a cell line oncogenic mouse model expressing a constitutively active NTRK1 mutation demonstrated decreased phosphorylation of Ntrk1 and inhibition of tumor growth when treated with Selitrectinib (LOXO-195) (PMID: 28578312). | 28578312 |
NTRK1 G613V | dedifferentiated liposarcoma | resistant | Selitrectinib | Preclinical - Cell culture | Actionable | In a preclinical study, a dedifferentiated liposarcoma cell line expressing NTRK1 G613V demonstrated resistance to Selitrectinib (LOXO-195) in culture (PMID: 38531265). | 38531265 |
NTRK2 fusion | Advanced Solid Tumor | predicted - sensitive | Selitrectinib | Phase I | Actionable | In a Phase I trial, Selitrectinib (LOXO-195) treatment resulted in an objective response rate of 34% (10/29) and stable disease in 31% (9/29) of adult and pediatric patients with advanced solid tumors harboring NTRK fusions and had progressed or were intolerant to prior Trk inhibitors (AACR Annual Meeting 2019, Abstract CT127; NCT03215511). | detail... |
NTRK1 G595R NTRK1 act mut | Advanced Solid Tumor | sensitive | Selitrectinib | Preclinical | Actionable | In a preclinical study, a cell line oncogenic mouse model expressing an NTRK1 activating mutation and a secondary resistance mutation, NTRK1 G595R, demonstrated sensitivity to Selitrectinib (LOXO-195) (PMID: 28578312). | 28578312 |
NTRK1 fusion | Advanced Solid Tumor | predicted - sensitive | Selitrectinib | Phase I | Actionable | In a Phase I trial, Selitrectinib (LOXO-195) treatment resulted in an objective response rate of 34% (10/29) and stable disease in 31% (9/29) of adult and pediatric patients with advanced solid tumors harboring NTRK fusions and had progressed or were intolerant to prior Trk inhibitors (AACR Annual Meeting 2019, Abstract CT127; NCT03215511). | detail... |
NTRK1 G667C NTRK1 act mut | Advanced Solid Tumor | sensitive | Selitrectinib | Preclinical | Actionable | In a preclinical study, a cell line oncogenic mouse model expressing an NTRK1 activating mutation and a secondary resistance mutation, NTRK1 G667C, was sensitive to treatment with Selitrectinib (LOXO-195), demonstrating inhibition of tumor growth (PMID: 28578312). | 28578312 |
NTRK2 fusion NTRK2 mut | Advanced Solid Tumor | predicted - sensitive | Selitrectinib | Phase I | Actionable | In a Phase I trial, Selitrectinib (LOXO-195) treatment resulted in an objective response rate of 45% (9/20) and stable disease in 30% (6/20) of adult and pediatric patients with advanced solid tumors harboring a NTRK mutation associated with resistance to TRK inhibitors in the context of NTRK fusions, who had progressed or were intolerant to prior Trk inhibitors (AACR Annual Meeting 2019, Abstract CT127; NCT03215511). | detail... |
NTRK1 H604Y NTRK1 G613V | dedifferentiated liposarcoma | resistant | Selitrectinib | Preclinical - Cell culture | Actionable | In a preclinical study, a dedifferentiated liposarcoma cell line expressing NTRK1 G613V and H604Y demonstrated resistance to Selitrectinib (LOXO-195) in culture (PMID: 38531265). | 38531265 |
NTRK1 fusion NTRK1 mut | Advanced Solid Tumor | predicted - sensitive | Selitrectinib | Phase I | Actionable | In a Phase I trial, Selitrectinib (LOXO-195) treatment resulted in an objective response rate of 45% (9/20) and stable disease in 30% (6/20) of adult and pediatric patients with advanced solid tumors harboring a NTRK mutation associated with resistance to TRK inhibitors in the context of NTRK fusions, who had progressed or were intolerant to prior Trk inhibitors (AACR Annual Meeting 2019, Abstract CT127; NCT03215511). | detail... |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
---|---|---|---|---|---|---|
NCT03215511 | Phase Ib/II | Selitrectinib | A Study to Test the Safety of the Investigational Drug Selitrectinib in Children and Adults That May Treat Cancer | Completed | USA | ITA | FRA | ESP | DEU | BEL | AUS | 3 |