ANTIBODY-DRUG CONJUGATE CONTAINING A HETEROCYCLIC COMPOUND THAT HAS AN INDUCTIVE EFFECT ON THE DEGRADATION OF THE MUTANT KRAS PROTEIN
Patent Information
- Application Number
- ARP20250100304
- Authority / Receiving Office
- AR · AR
- Patent Type
- Applications
- Current Assignee / Owner
- Priority Date
- 2024-02-05
- Filing Date
- 2025-02-04
- Publication Date
- 2026-07-08
Claims
An antibody-drug conjugate is provided for use in the treatment of cancer expressing mutant KRAS, in particular, mutant KRAS G12V, mutant G12D, and mutant G12C. A drug and a drug-linker conjugate for use in the antibody-drug conjugate are also provided. The present inventors have conjugated a heterocyclic compound that induces the degradation of mutant KRAS protein, the heterocyclic compound being represented by formula (2), with an anti-EGFR antibody to prepare an antibody-drug conjugate capable of delivering the compound to a type of cancer expressing EGFR. Furthermore, a drug-linker conjugate for use in the antibody-drug conjugate or a salt thereof has been found.The antibody-drug conjugate inhibits mutant KRAS by inducing the degradation of mutant KRAS, in particular, mutant KRAS protein G12V, mutant G12D and mutant G12C, in a type of cancer that expresses EGFR, and exhibits an antitumor effect.