Drug intelligence / Profile preview

salirasib

Development stage
Phase 2
Lead developer
Advanz Pharma
Modality
Small Molecules
Administration
Oral
01

Overview

Salirasib is a small molecule and a salicylic acid derivative with potential antineoplastic activity. It acts as an oral RAS inhibitor by mimicking the c-terminal farnesyl cysteine common to all RAS isoforms, thereby competing with farnesylated RAS for binding sites on the plasma membrane. This disrupts the membrane association of active GTP-bound RAS proteins, leading to their degradation and inhibition of downstream signaling pathways involved in cell proliferation, differentiation, and senescence. Salirasib also inhibits mTOR complex 1 activity by disrupting the mTOR-raptor complex. It has been investigated primarily for cancers characterized by RAS mutations (such as non-small cell lung cancer and pancreatic cancer), but clinical trials have shown limited efficacy in KRAS mutant lung adenocarcinoma[1][3][6][7][8].

Other names
farnesylthiosalicylic acid
02

Targets

HMGB1 (High mobility group protein B1)Mechanistic target of rapamycin complex 1

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