Drug intelligence / Profile preview

inlexisertib + trametinib

Development stage
Unknown
Lead developer
Deciphera Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Inlexisertib + trametinib is an experimental oral combination regimen designed for the treatment of patients with **advanced or metastatic solid tumors** that harbor RAS/MAPK pathway mutations. **Inlexisertib** (code name: DCC-3116) is a first-in-human, orally bioavailable small molecule inhibitor of ULK1/2, which are central regulators of autophagy—a pathway often upregulated as a survival strategy in RAS/MAPK-altered cancers. **Trametinib** is a selective small molecule inhibitor of MEK1/2, downstream kinases in the MAPK pathway. Preclinical rationale suggests that dual inhibition of autophagy (via ULK1/2) and MAPK signaling (via MEK inhibition) may overcome resistance mechanisms and enhance antitumor effects. The combination is currently under investigation in Phase 1/2 clinical trials for patients with RAS/MAPK pathway mutant solid tumors, including but not limited to pancreatic, rectal, and colon cancer[3][6].

Other names
DCC-3116 + trametinib
02

Targets

MEK2 (Dual specificity mitogen-activated protein kinase kinase 2)ULK2 (Unc-51-like kinase 2)MEK1 (Dual specificity mitogen-activated protein kinase kinase 1)

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