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Association details:
| Biomarker: | NRAS mutation |
|---|---|
| Cancer: | Melanoma |
| Drug: | exarafenib (KIN-2787) (pan-RAF inhibitor) |
| Direction: | Sensitive |
Evidence:
Source:
Title:
Kinnate Biopharma Inc. Receives Fast Track Designation from the U.S. Food and Drug Administration for KIN-2787, an Investigational Pan-RAF Inhibitor
Published date:
09/21/2022
Excerpt:
Kinnate Biopharma Inc. (Nasdaq: KNTE) (“Kinnate”), a clinical-stage precision oncology company, today announced that the U.S. Food and Drug Administration (FDA) has granted Fast Track designation for Kinnate’s investigational pan-RAF inhibitor, KIN-2787, for treatment of patients with BRAF Class II or III alteration-positive and/or NRAS mutation-positive stage IIb to IV malignant melanoma that is metastatic or unresectable.
Source:
Title:
A Study to Evaluate KIN-2787 in Participants With BRAF and/or NRAS Mutation Positive Solid Tumors
Excerpt:
...- Known BRAF Class I, Class II, or Class III alteration or melanoma with an NRAS mutation as confirmed by previous genomic analysis of tumor tissue or ctDNA....
Trial ID:
Source:
Title:
4927 / 5 - Exarafenib (KIN-2787) is a potent, selective pan-RAF inhibitor with activity in preclinical models of BRAF class II/III mutant and NRAS mutant melanoma
Published date:
03/15/2023
Excerpt:
In vivo KIN-2787 efficacy was evaluated in cell line-derived xenograft (CDX) and patient-derived xenograft (PDX) models of human BRAF and NRAS mutant cancer….treatment with exarafenib demonstrated significant tumor growth inhibition at 30 mg/kg BID in CDX and PDX models of human NRAS mutant melanoma....In addition to efficacy in BRAF mutant tumors, these data support use of exarafenib in combination therapy with MEK inhibitors in NRAS mutant melanoma.
Source:
Title:
2674 / 17 - Antitumor activity of KIN-2787, a next-generation pan-RAF inhibitor, in preclinical models of human RAF/RAS mutant melanoma
Published date:
03/09/2022
Excerpt:
KIN-2787 activity was assessed by suppression of downstream MAPK pathway signaling and subsequent cell growth inhibition in a panel of human melanoma cell lines. In vivo KIN-2787 efficacy was evaluated in BRAF and NRAS mutant melanoma cell- and patient-derived xenograft models.RAS and KRAS mutant cell lines were moderately responsive to KIN-2787 inhibition. Melanoma cells expressing wild type RAS/RAF were the least sensitive to MAPK pathway inhibition by KIN-2787. KIN-2787 is a next-generation, pan-RAF inhibitor with in vitro and in vivo activity against human melanoma driven by BRAF and/or NRAS mutations. Data supports KIN-2787 use in acquired BRAF dimer-dependent resistance to BRAF+MEK inhibitor therapy
