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| Therapy Name | IDRX-42 |
| Synonyms | |
| Therapy Description |
IDRX-42 is a KIT inhibitor, which potentially decreases tumor cell viability and reduces tumor growth (PMID: 40018846). |
| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| IDRX-42 | M-4205|M 4205|M4205|IDRX 42|IDRX42 | KIT Inhibitor 57 | IDRX-42 is a KIT inhibitor, which potentially decreases tumor cell viability and reduces tumor growth (PMID: 40018846). |
| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| KIT V559D | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT V559D in an vitro assay (PMID: 40018846). | 40018846 |
| KIT T670I | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT T670I in an vitro assay (PMID: 40018846). | 40018846 |
| KIT D816F | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT D816F in an vitro assay (PMID: 40018846). | 40018846 |
| KIT D820E | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT D820E in an vitro assay (PMID: 40018846). | 40018846 |
| KIT D816V | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT D816V in an vitro assay (PMID: 40018846). | 40018846 |
| KIT D816E | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT D816E in an vitro assay (PMID: 40018846). | 40018846 |
| KIT D820Y | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT D820Y in an vitro assay (PMID: 40018846). | 40018846 |
| KIT W557_K558del | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT W557_K558del in an vitro assay (PMID: 40018846). | 40018846 |
| KIT W557_K558del | gastrointestinal stromal tumor | sensitive | IDRX-42 | Preclinical - Pdx | Actionable | In a preclinical study, IDRX-42 induced tumor regression in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT W557_K558del (PMID: 40018846). | 40018846 |
| FLT3 exon 14 ins | acute myeloid leukemia | sensitive | IDRX-42 | Preclinical - Cell culture | Actionable | In a preclinical study, IDRX-42 inhibited viability of acute myeloid leukemia cell lines harboring FLT3-ITD in culture (PMID: 40018846). | 40018846 |
| KIT W557_K558del KIT V654A | gastrointestinal stromal tumor | sensitive | IDRX-42 | Preclinical - Pdx | Actionable | In a preclinical study, IDRX-42 treatment led to a complete response in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT W557_K558del and KIT V654A (PMID: 40018846). | 40018846 |
| KIT V560G KIT D816V | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT V560G and KIT D816V in an vitro assay (PMID: 40018846). | 40018846 |
| KIT Y823D | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT Y823D in an vitro assay (PMID: 40018846). | 40018846 |
| KIT A829P | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT A829P in an vitro assay (PMID: 40018846). | 40018846 |
| KIT V560G | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT V560G in an vitro assay (PMID: 40018846). | 40018846 |
| KIT D816I | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT D816I in an vitro assay (PMID: 40018846). | 40018846 |
| KIT V559D KIT T670I | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT V559D and KIT T670I in an vitro assay (PMID: 40018846). | 40018846 |
| KIT W557Lfs*5 KIT P577del KIT D820G | gastrointestinal stromal tumor | predicted - sensitive | IDRX-42 | Preclinical - Pdx | Actionable | In a preclinical study, IDRX-42 treatment inhibited mitosis and decreased tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT P577del, W557Lfs*5, and D820G (PMID: 37223931). | 37223931 |
| KIT V654A | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT V654A in an vitro assay (PMID: 40018846). | 40018846 |
| KIT V560_Y578del | gastrointestinal stromal tumor | sensitive | IDRX-42 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, IDRX-42 inhibited viability of a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del in culture, and induced tumor regression in a cell line xenograft model (PMID: 40018846). | 40018846 |
| KIT W557_V559delinsF | gastrointestinal stromal tumor | sensitive | IDRX-42 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, IDRX-42 inhibited viability of a gastrointestinal stromal tumor cell line harboring KIT W557_V559delinsF in culture, and induced tumor regression in a patient-derived xenograft (PDX) model (PMID: 40018846). | 40018846 |
| KIT V559D KIT V654A | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT V559D and KIT V654A in an vitro assay (PMID: 40018846). | 40018846 |
| KIT K642E | gastrointestinal stromal tumor | predicted - sensitive | IDRX-42 | Preclinical - Pdx | Actionable | In a preclinical study, IDRX-42 treatment inhibited mitosis and decreased tumor growth in a cell line xenograft model and a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT K642E (PMID: 37223931). | 37223931 |
| KIT V560_Y578del KIT V654A | gastrointestinal stromal tumor | sensitive | IDRX-42 | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, IDRX-42 inhibited viability of a gastrointestinal stromal tumor cell line harboring KIT V560_Y578del and KIT V654A in culture, and resulted in tumor shrinkage in a cell line xenograft model and a complete response in a patient-derived xenograft (PDX) model (PMID: 40018846). | 40018846 |
| KIT V559A | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT V559A in an vitro assay (PMID: 40018846). | 40018846 |
| KIT exon9 | gastrointestinal stromal tumor | predicted - sensitive | IDRX-42 | Phase I | Actionable | In a Phase I trial, IDRX-42 treatment demonstrated safety and resulted in 9 partial responses among 39 evaluable patients with gastrointestinal stromal tumors harboring a KIT exon 11 (n=27), exon 9 (n=13), or exon 8 (n=2) mutation with a clinical benefit rate of 71% overall and 100% as second-line treatment (J Clin Oncol 42, 2024 (suppl 16; abstr 11501); NCT05489237). | detail... |
| KIT A502_Y503dup | gastrointestinal stromal tumor | predicted - sensitive | IDRX-42 | Preclinical - Pdx | Actionable | In a preclinical study, IDRX-42 treatment inhibited mitosis and decreased tumor growth in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT A502_Y503dup (PMID: 37223931). | 37223931 |
| KIT K642E | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT K642E in an vitro assay (PMID: 40018846). | 40018846 |
| KIT exon11 | gastrointestinal stromal tumor | predicted - sensitive | IDRX-42 | Phase I | Actionable | In a Phase I trial, IDRX-42 treatment demonstrated safety and resulted in 9 partial responses among 39 evaluable patients with gastrointestinal stromal tumor harboring a KIT exon 11 (n=27), exon 9 (n=13), or exon 8 (n=2) mutation with a clinical benefit rate of 71% overall and 100% as second-line treatment (J Clin Oncol 42, 2024 (suppl 16; abstr 11501); NCT05489237). | detail... |
| KIT V560G KIT N822K | Advanced Solid Tumor | predicted - sensitive | IDRX-42 | Preclinical - Biochemical | Actionable | In a preclinical study, IDRX-42 inhibited kinase activity of KIT V560G and KIT N822K in an vitro assay (PMID: 40018846). | 40018846 |
| KIT N822K | acute myeloid leukemia | sensitive | IDRX-42 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, IDRX-42 inhibited viability of an acute myeloid leukemia cell line harboring KIT N822K in culture, and induced tumor regression in a cell line xenograft model (PMID: 40018846). | 40018846 |
| KIT W557_K558del KIT Y823D | gastrointestinal stromal tumor | sensitive | IDRX-42 | Preclinical - Pdx | Actionable | In a preclinical study, IDRX-42 treatment resulted in tumor shrinkage in a patient-derived xenograft (PDX) model of gastrointestinal stromal tumor harboring KIT W557_K558del and KIT Y823D (PMID: 40018846). | 40018846 |
| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT05489237 | Phase I | IDRX-42 | A First-in-human (FIH) Study of IDRX-42 in Participants With Metastatic and/or Unresectable Gastrointestinal Stromal Tumors (GIST) [Study ID: StrateGIST 1] | Recruiting | USA | NLD | ITA | GBR | FRA | ESP | DEU | BEL | 3 |