Drug intelligence / Profile preview

befotertinib + rifampicin

Development stage
Phase 1
Lead developer
Betta Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Befotertinib + rifampicin is a drug-drug interaction study regimen evaluated in a Phase 1 clinical trial. Befotertinib (brand name: Surmana) is an orally administered, highly selective, irreversible, third-generation small molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) developed by Betta Pharmaceuticals and InventisBio. It is approved in China for the treatment of EGFR T790M mutation-positive non-small cell lung cancer (NSCLC). Rifampicin is a potent inducer of cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp) via activation of the pregnane X receptor (PXR). In this clinical trial, rifampicin is not used as a therapeutic co-drug but rather as a probe agent to evaluate the impact of strong CYP3A4 induction on the pharmacokinetics, safety, and tolerability of befotertinib in healthy participants.

Other names
D-0316 + rifampicinD-0316 + rifampinSurmana + Rifadinbefotertinib + rifampinbefotertinib and rifampicinbefotertinib and rifampin
02

Targets

ABCG2 (Breast cancer resistance protein)EGFR (Epidermal growth factor receptor)

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