Drug intelligence / Profile preview

OB-001 + osimertinib

Development stage
Preclinical
Lead developer
OncoBayes
Modality
Small Molecules
Administration
Oral
01

Overview

OB-001 + osimertinib is an investigational combination therapy being developed by OncoBayes for the treatment of EGFR-mutant non-small cell lung cancer (NSCLC), particularly for patients with central nervous system (CNS) metastases. OB-001 is a proprietary amorphous solid dispersion formulation of elacridar, produced using KinetiSol technology to overcome the poor bioavailability of crystalline elacridar. It acts as a highly selective inhibitor of the efflux transporters P-glycoprotein (P-gp) and Breast Cancer Resistance Protein (BCRP) at the blood-brain barrier (BBB). Osimertinib is an approved, third-generation, irreversible EGFR tyrosine kinase inhibitor. By inhibiting P-gp and BCRP, OB-001 prevents the efflux of osimertinib at the BBB, thereby significantly enhancing its brain delivery and therapeutic efficacy against CNS metastases without increasing systemic exposure.

Other names
OB-001 + AZD9291OB-001 and osimertinibOB001 and osimertinibOB 001 and osimertinibelacridar + AZD9291elacridar + osimertinibelacridar and osimertinib
02

Targets

ABCB1 (P-glycoprotein)ABCG2 (Breast cancer resistance protein)EGFR (Epidermal growth factor receptor)

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