Therapy Detail

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Therapy Name LXH 254 + Trametinib
Synonyms
Therapy Description

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Drug Name Trade Name Synonyms Drug Classes Drug Description
LXH 254 LXH254|LXH-254|Naporafenib BRAF Inhibitor 22 CRAF Inhibitor 11 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).
Trametinib Mekinist GSK1120212 MEK inhibitor (Pan) 23 MEK1 Inhibitor 25 MEK2 Inhibitor 23 Mekinist (trametinib) inhibits MEK 1 and 2, which potentially leads to reduced tumor cell proliferation (PMID: 27956260). Mekinist (trametinib) is FDA approved for melanoma patients harboring BRAF V600E or BRAF V600K mutations, and in combination with Tafinlar (dabrafenib) for BRAF V600E/K-mutant melanoma, BRAF V600E- mutant non-small cell lung cancer, BRAF V600E-mutant anaplastic thyroid cancer, for adult and pediatric patients of 6 years or older with unresectable or metastatic solid tumors harboring BRAF V600E, and for pediatric patients of 1 year or older with low-grade glioma harboring BRAF V600E (FDA.gov).

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  • Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
NRAS Q61R urinary bladder cancer sensitive LXH 254 + Trametinib Preclinical - Cell line xenograft Actionable In a preclinical study, LXH 254 and Mekinist (trametinib) combination treatment decreased tumor volume and weight compared to vehicle in a cell line xenograft model of bladder cancer harboring NRAS Q61R (PMID: 34554931). 34554931
NRAS mutant melanoma predicted - sensitive LXH 254 + Trametinib Phase I Actionable In a Phase Ib trial, combination treatment with LXH 254 and Mekinist (trametinib) resulted in an overall response rate of 30% (9/30) and stable disease in 43.3% (13/30) of patients with melanoma harboring NRAS mutations (Cancer Res 2022;82(12_Suppl):Abstract nr CT197; NCT02974725). detail...

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  • Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
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  • Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")

Sorting

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries
NCT02974725 Phase I LXH 254 + Ribociclib LXH 254 + Trametinib LTT462 + LXH 254 A Phase Ib Study of LXH254-centric Combinations in NSCLC or Melanoma Active, not recruiting USA | ITA | FRA | ESP | DEU | BEL 5


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