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Therapy Name | KIN-3248 |
Synonyms | |
Therapy Description |
KIN-3248 is a small molecule pan-FGFR inhibitor with activity against secondary resistance mutations, potentially inhibiting tumor growth (J Clin Oncol 40, 2022 (suppl 4; abstr 461)). |
Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
---|---|---|---|---|
KIN-3248 | KIN3248|KIN 3248 | FGFR Inhibitor (Pan) 26 | KIN-3248 is a small molecule pan-FGFR inhibitor with activity against secondary resistance mutations, potentially inhibiting tumor growth (J Clin Oncol 40, 2022 (suppl 4; abstr 461)). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|
FGFR3 K650M | Advanced Solid Tumor | predicted - sensitive | KIN-3248 | Preclinical - Biochemical | Actionable | In a preclinical study, KIN-3248 inhibited kinase activity of FGFR3 K650M in an in vitro assay (PMID: 38437671). | 38437671 |
FGFR3 S249C FGFR3 N540K | urinary bladder cancer | sensitive | KIN-3248 | Preclinical - Cell culture | Actionable | In a preclinical study, KIN-3248 inhibited viability of a bladder cancer cell line harboring FGFR3 S249C and expressing FGFR3 N540K in culture (PMID: 38437671). | 38437671 |
FGFR3 S249C FGFR3 V555M | urinary bladder cancer | sensitive | KIN-3248 | Preclinical - Cell culture | Actionable | In a preclinical study, KIN-3248 inhibited viability of a bladder cancer cell line harboring FGFR3 S249C and expressing FGFR3 V555M in culture (PMID: 38437671). | 38437671 |
FGFR2 N550H | Advanced Solid Tumor | predicted - sensitive | KIN-3248 | Preclinical - Biochemical | Actionable | In a preclinical study, KIN-3248 inhibited kinase activity of FGFR2 N550H in an in vitro assay (PMID: 38437671). | 38437671 |
FGFR2 fusion | gastroesophageal junction adenocarcinoma | predicted - sensitive | KIN-3248 | Phase I | Actionable | In a Phase I trial, KIN-3248 treatment demonstrated safety and preliminary activity in patients with advanced solid tumors harboring alterations in FGFR2 or FGFR3, with an objective response rate of 9.25% (5/54, 5 partial responses (PR)), including 2 PRs in patients with gastroesophageal jucntion cancer harboring a FGFR2 fusion (PMID: 38602417; NCT05242822). | 38602417 |
FGFR2 G542A FGFR2 V564L FGFR2 amp | stomach cancer | sensitive | KIN-3248 | Preclinical - Pdx | Actionable | In a preclinical study, KIN-3248 treatment inhibited tumor growth in a gastric cancer patient derived xenograft (PDX) model harboring FGFR2 V564L and G542A with FGFR2 amplification (PMID: 38267212). | 38267212 |
FGFR2 act mut | Advanced Solid Tumor | predicted - sensitive | KIN-3248 | Phase I | Actionable | In a Phase I trial, KIN-3248 treatment demonstrated safety and preliminary activity in patients with advanced solid tumors harboring alterations in FGFR2 or FGFR3, resulting in an objective response rate of 9.25% (5/54, 5 partial responses) and disease control rate of 46% (25/54), with stable disease in 20 patients (PMID: 38602417; NCT05242822). | 38602417 |
FGFR3 act mut | Advanced Solid Tumor | predicted - sensitive | KIN-3248 | Phase I | Actionable | In a Phase I trial, KIN-3248 treatment demonstrated safety and preliminary activity in patients with advanced solid tumors harboring alterations in FGFR2 or FGFR3, resulting in an objective response rate of 9.25% (5/54, 5 partial responses) and disease control rate of 46% (25/54), with stable disease in 20 patients (PMID: 38602417; NCT05242822). | 38602417 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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NCT05242822 | Phase I | KIN-3248 | A Study to Evaluate KIN-3248 in Participants With Advanced Tumors Harboring FGFR2 and//or FGFR3 Gene Alterations | Active, not recruiting | USA | ESP | DNK | 3 |