ANTIBODY-DRUG CONJUGATE CONTAINING A HETEROCYCLIC COMPOUND THAT HAS AN INDUCTIVE EFFECT ON THE DEGRADATION OF THE MUTANT KRAS PROTEIN

AR135173A1Pending Publication Date: 2026-07-08ASTELLAS PHARMA INC
View PDF 0 Cites 0 Cited by

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
Patent Text Reader
Need to check novelty before this filing date? Find Prior Art
No text content released.

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.