Drug intelligence / Profile preview

bgb-53038 + cetuximab

Development stage
Unknown
Lead developer
BeOne Medicines
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

**bgb-53038 + cetuximab** is an investigational combination therapy under evaluation for the treatment of advanced or metastatic solid tumors—most notably colorectal cancer—with KRAS mutations or amplification. BGB-53038 is a small molecule pan-KRAS inhibitor that targets KRAS, a key oncogenic driver in multiple cancers, by inhibiting its GTPase activity. Cetuximab is a monoclonal antibody against the epidermal growth factor receptor (EGFR), used in various solid malignancies. The rationale for this combination is to inhibit parallel tumor-driving pathways, potentially enhancing antitumor activity in KRAS-driven cancers that may not sufficiently respond to KRAS inhibition alone. The combination is currently in phase 1 clinical trials, with the sponsors assessing its safety, pharmacokinetics, and preliminary efficacy in patients with KRAS-mutant or amplified solid tumors, particularly colorectal cancer. The drugs are administered intravenously[1][3].

Other names
BGB 53038 + cetuximab
02

Targets

EGFR T790M (Epidermal growth factor receptor T790M mutant)KRAS (Kirsten rat sarcoma viral oncogene homolog)

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