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adagrasib + afatinib
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Combination therapy of **adagrasib** (a selective, irreversible inhibitor of KRAS G12C mutation; developed primarily for advanced solid tumors) and **afatinib** (an irreversible pan-ERBB and EGFR family tyrosine kinase inhibitor), being studied for synergistic antitumor effects and overcoming resistance to KRAS inhibition[1][3][6]. Adagrasib blocks mutant KRAS signaling; afatinib binds nonreversibly to the ERBB receptor family, broadly inhibiting EGFR, HER2, and related pathways to prevent compensatory resistance. Together, this dual inhibition more effectively clears tumors and prevents/drives regression of resistance, notably in preclinical pancreatic cancer models[1]. No marketed combination product; clinical investigation is ongoing[1][3].
- Brand names
- Krazati (adagrasib)Gilotrif (afatinib)
- Other names
- adagrasib + afatinib
02
Targets
KRASG12C (Kirsten rat sarcoma viral oncogene homolog G12C)ERBB2 (Erb-b2 receptor tyrosine kinase 2)EGFR T790M (Epidermal growth factor receptor T790M mutant)ERBB4 (Erb-b2 receptor tyrosine kinase 4)
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