Drug intelligence / Profile preview

pp-121

Development stage
Preclinical
Lead developer
REVOLUTION Medicines
Modality
Small Molecules
01

Overview

PP-121 is a small molecule experimental drug that acts as a dual inhibitor of receptor tyrosine kinases (RTKs) and phosphoinositide 3-kinase (PI3K) family kinases. It potently inhibits the proliferation of certain tumor cell lines by directly targeting PI3Ks and mTOR, and also blocks RTKs such as Abl, Src, VEGFR-2, and PDGFR[4][1][5]. PP-121 has demonstrated anticancer activity in preclinical models by suppressing cell viability, inducing apoptosis, inhibiting cell migration and invasion in anaplastic thyroid carcinoma (ATC), non-small cell lung cancer (NSCLC), and other tumor types[5][7]. Additionally, it has shown anti-contractile and anti-inflammatory effects in asthma models by blocking ion channels involved in airway smooth muscle contraction and downregulating inflammatory pathways[2]. The drug is not approved for any indication.

02

Targets

ABL1 (ABL proto-oncogene 1, non-receptor tyrosine kinase)DNA-PK (DNA-dependent protein kinase)EGFR (Epidermal growth factor receptor)EPHB4 (Ephrin type-B receptor 4)HCK (Haematopoietic Cell Kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PIK3CA (Phosphoinositide 3-kinase alpha)PIK3CB (Phosphatidylinositol 3-kinase beta subunit)PIK3CG (Phosphatidylinositol 4,5-bisphosphate 3-kinase gamma)PIK3CD (Phosphatidylinositol 3-kinase delta)RET (Rearranged during transfection receptor tyrosine kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)VEGFR2 (Vascular endothelial growth factor receptor 2)Mechanistic target of rapamycin kinase complex 2

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