Therapy Detail

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Therapy Name LXH 254
Synonyms
Therapy Description

LXH 254 is a RAF inhibitor that selectively inhibits monomeric and dimerized BRAF and CRAF, which may lead to anti-tumor activity in RAF-mutant tumors and better tolerability (AACR Annual Meeting 2019, Abstract LB-114, PMID: 31059256).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
LXH 254 LXH254|LXH-254|Naporafenib BRAF Inhibitor 25 CRAF Inhibitor 12 LXH 254 is a RAF inhibitor that selectively inhibits monomeric and dimerized BRAF and CRAF, which may lead to anti-tumor activity in RAF-mutant tumors and better tolerability (AACR Annual Meeting 2019, Abstract LB-114, PMID: 31059256).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
BRAF G469A lung adenocarcinoma sensitive LXH 254 Preclinical - Patient cell culture Actionable In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF G469A were sensitive to treatment with LXH 254 in culture, demonstrating inhibition of cell growth (PMID: 32540409). 32540409
HRAS G12V urinary bladder cancer sensitive LXH 254 Preclinical - Cell culture Actionable In a preclinical study, LXH 254 treatment decreased viability of a bladder cancer cell line harboring HRAS G12V in culture (PMID: 34554931). 34554931
BRAF loss NRAS Q61K melanoma decreased response LXH 254 Preclinical - Cell culture Actionable In a preclinical study, CRISPR-Cas9 mediated knockout of BRAF in a melanoma cell line harboring NRAS Q61K led to decreased sensitivity to LXH254 treatment compared to parental cells harboring BRAF D287H and NRAS Q61K in culture (PMID: 33355204). 33355204
BRAF L485_T488delinsF Advanced Solid Tumor predicted - sensitive LXH 254 Preclinical - Biochemical Actionable In a preclinical study, LXH 254 inhibited ERK and MEK signaling in cells expressing BRAF L485_T488delinsF in culture (PMID: 37656784). 37656784
BRAF L597V lung adenocarcinoma sensitive LXH 254 Preclinical - Patient cell culture Actionable In a preclinical study, cells derived from a lung adenocarcinoma patient harboring BRAF L597V were sensitive to treatment with LXH 254 in culture, demonstrating inhibition of cell growth (PMID: 32540409). 32540409
BRAF mutant Advanced Solid Tumor predicted - sensitive LXH 254 Case Reports/Case Series Actionable In a Phase I trial, LXH 254 treatment resulted in partial response in 2.6% (2/75) and stable disease in 33% (25/75) of patients with advanced solid tumors harboring MAPK pathway alterations, one of the patient achieved partial response harbored a BRAF mutation (J Clin Oncol 36, no. 15_suppl (May 20 2018) 2586-2586; NCT02607813). detail...
NRAS Q61R urinary bladder cancer sensitive LXH 254 Preclinical - Cell line xenograft Actionable In a preclinical study, LXH 254 treatment decreased Mek signaling, colony formation and viability, and increased apoptosis in a bladder cancer cell line harboring NRAS Q61R in culture and decreased tumor weight and volume in a cell line xenograft model (PMID: 34554931). 34554931
BRAF V600E melanoma predicted - sensitive LXH 254 Preclinical - Cell line xenograft Actionable In a preclinical study, a melanoma cell line harboring BRAF V600E was sensitive to treatment with LXH254, demonstrating inhibition of cell proliferation in culture, and inhibition of tumor growth and tumor regression in a cell line xenograft model of melanoma (PMID: 33355204). 33355204
BRAF D287H NRAS Q61K melanoma predicted - sensitive LXH 254 Preclinical - Cell line xenograft Actionable In a preclinical study, a melanoma cell line harboring BRAF D287H and NRAS Q61K was sensitive to treatment with LXH254, demonstrating inhibition of cell proliferation in culture, and inhibition of tumor growth in a cell line xenograft model of melanoma (PMID: 33355204). 33355204

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT02607813 Phase I LXH 254 + Spartalizumab LXH 254 Phase I Study of LXH254 in Patients With Advanced Solid Tumors Haboring MAPK Pathway Alterations Terminated USA | ITA | FRA | ESP | DEU | CAN 4


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