Crystalline Forms of Orally Available Selective KIT and PDGFR Kinase Inhibitor

ChangeBridge: Patent Grants - Organic Chemistry (C07D)

Published March 31st, 2026

Detected March 31st, 2026

Summary

USPTO granted patent US12590095B2 to Sandoz AG on March 31, 2026, covering crystalline forms of avapritinib, a KIT and PDGFR kinase inhibitor. The patent (CPC C07D 487/04) protects polymorphs and hydrates of the compound for treating gastrointestinal stromal tumors (GIST) and advanced systemic mastocytosis (AdvSM). Inventors include Verena Adamer, Andrea Thaler, and Erwin Schreiner.

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What changed

USPTO issued Patent No. US12590095B2 to Sandoz AG granting exclusive rights to crystalline avapritinib polymorphs, hydrates, and pharmaceutical compositions containing these forms. The patent covers methods of treatment for GIST and advanced systemic mastocytosis including aggressive systemic mastocytosis (ASM), SM-AHN, and mast cell leukemia (MCL). The patent application (No. 17625138) was filed on July 2, 2020, and contains 15 claims.

This patent grant does not impose compliance obligations on other pharmaceutical companies. Generic manufacturers seeking to produce avapritinib formulations must design around these crystal forms or await patent expiration. Freedom-to-operate analyses should consider this patent alongside other Orange Book-listed patents for avapritinib (e.g., US10975095B2) when evaluating market entry strategies.

Source document (simplified)

← USPTO Patent Grants

Crystalline forms of an orally available, selective kit and PDGFR kinase inhibitor

Grant US12590095B2 Kind: B2 Mar 31, 2026

Assignee

SANDOZ AG

Inventors

Verena Adamer, Andrea Thaler, Erwin Schreiner

Abstract

The present invention relates to crystalline avapritinib, polymorphs and hydrates thereof as well as to processes for their preparation. Furthermore, the invention relates to a pharmaceutical composition comprising crystalline avapritinib and at least one pharmaceutically acceptable excipient. The pharmaceutical composition of the present invention can be used as a medicament, in particular for the treatment of patients with gastrointestinal stromal tumors (GIST) and advanced systemic mastocytosis (AdvSM), including aggressive systemic mastocytosis (ASM), systemic mastocytosis with an associated hematologic neoplasm (SM-AHN) and mast cell leukemia (MCL).