A patent review of mutant-selective PI3Kα inhibitors for the treatment of different cancers (2021-2025).

doi:10.1080/13543776.2026.2704853

Loading publication...

Noodle always counts identifier-free feature events for service operation. With your permission, Google Analytics can also estimate audience and engagement. Search text, publication identifiers, cookies, IP addresses and browser fingerprints are never included in Noodle's first-party event counters.

Privacy details

Community

Back to search

Article

A patent review of mutant-selective PI3Kα inhibitors for the treatment of different cancers (2021-2025).

Expert opinion on therapeutic patents - 1 Sept 2026

Qi Haixiang, Wen Jiayang, Xu Heng

Abstract excerpt

INTRODUCTION: Oncogenic PIK3CA mutations drive numerous solid tumors, rendering PI3Kα a key therapeutic target. However, conventional ATP-competitive inhibitors are severely limited by dose-limiting metabolic toxicities caused by wild-type PI3Kα inhibition. To circumvent these limitations, the drug discovery landscape is rapidly shifting toward mutant-selective allosteric inhibitors designed to spare...

Read the complete abstract on PubMed

Topics

Humans
Patents as Topic
Neoplasms
Animals
Antineoplastic Agents
Mutation
Phosphoinositide-3 Kinase Inhibitors

Methodology Data sources Editorial policy Privacy Delete account & data About Contact Helena Bioinformatics

Class I Phosphatidylinositol 3-Kinases

Drug Discovery

Allosteric Regulation

Drug Resistance, Neoplasm

Proteolysis Targeting Chimera

Drug Development

Drug Design

Source

Open in PubMed

Identifiers

PMID: 42508941
DOI: 10.1080/13543776.2026.2704853

Genes

PIK3CA

Provenance

PubMed metadata and Literature Corpus relationships. Corpus snapshot updated 24 Oct 2026.

Related research

Semantic proximity does not establish scientific evidence. Graph snapshot: 2026-09-29.

Research trail→

Click a neighbor to travelStep 1 · 12 closest

A patent review of mutant-selective PI3Kα inhibitors for the treatment of different cancers (2021-2025).PMID 42508941Read ↗

Structural Insights into the Development of Inhibitors Against Cancer-Specific Mutations of PI3Kα.Semantic proximity Read ↗

Phosphatidylinositol 3-kinase (PI3K) inhibitors: a recent update on inhibitor design and clinical trials (2016-2020).Semantic proximity Read ↗

Discovery of Pyridopyrimidinones that Selectively Inhibit the H1047R PI3Kα Mutant Protein.Semantic proximity Read ↗

Somatic mutations in PI3Kα: Structural basis for enzyme activation and drug designSemantic proximity Read ↗

The emerging role of PI3K inhibitors for solid tumour treatment and beyond.Semantic proximity Read ↗

High-throughput screening campaigns against a PI3Kα isoform bearing the H1047R mutation identified potential inhibitors with novel scaffolds.Semantic proximity Read ↗

Strategies and techniques for preclinical therapeutic targeting of PI3K in oncology: where do we stand in 2024?Semantic proximity Read ↗

Kinase Inhibitor Profiling Reveals Unexpected Opportunities to Inhibit Disease-Associated Mutant Kinases.Semantic proximity Read ↗

Drugging the PI3 Kinome: From Chemical Tools to Drugs in the ClinicSemantic proximity Read ↗

Precision Targeting of Mutant PI3Kα.Semantic proximity Read ↗

Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα.Semantic proximity Read ↗

Structure, function and inhibition of the phosphoinositide 3-kinase p110α enzyme.Semantic proximity Read ↗

⌁Select a neighboring publication to make it the new centre.