Research map: A patent review of mutant-selective PI3Kα inhibitors for the treatment of different cancers (2021–2025)

Back to the article

Papers in this map

  1. High Frequency of Mutations of the PIK3CA Gene in Human Cancers · Yardena Samuels · 2004 · 3473 citations · Cited by this paper
  2. Sirtuin modulators: a review of patents from 2020 to 2024 · 2025 · Related
  3. PROTAC targeted protein degraders: the past is prologue · Miklós Békés · 2022 · 3299 citations · Cited by this paper
  4. A patent review of Mpro protease inhibitors for the treatment of COVID-19 infections (2020 – present) · 2025 · Related
  5. The PI3K Pathway in Human Disease · David A. Fruman · 2017 · 2812 citations · Cited by this paper
  6. Therapeutic applications of benzoxaborole compounds: a patent and literature analysis (2019–2024) · 2025 · Related
  7. Alpelisib for PIK3CA -Mutated, Hormone Receptor–Positive Advanced Breast Cancer · Fabrice André · 2019 · 2663 citations · Cited by this paper
  8. An updated patent review of histone deacetylase 6 inhibitors in neurodegenerative diseases (2020–2025) · 2026 · Related
  9. The emerging mechanisms of isoform-specific PI3K signalling · Bart Vanhaesebroeck · 2010 · 1776 citations · Cited by this paper
  10. 5’-Ectonucleotidase (CD73) inhibitors: a patent review (2021-present) · 2026 · Related
  11. Idelalisib and Rituximab in Relapsed Chronic Lymphocytic Leukemia · Richard R. Furman · 2014 · 1708 citations · Cited by this paper
  12. PCSK9 inhibitors: an updated patent review 2024–2025 · 2026 · Related
  13. PI3K in cancer: divergent roles of isoforms, modes of activation and therapeutic targeting · Lauren M. Thorpe · 2014 · 1386 citations · Cited by this paper
  14. Topoisomerase II inhibitors in oncology: an updated patent review (2016-present) · 2025 · Related
  15. PI3K in lymphocyte development, differentiation and activation · Klaus Okkenhaug · 2003 · 824 citations · Cited by this paper
  16. Recent advances in the discovery of PKMYT1-targeting drugs: a patent review (2021–2025) · 2026 · Related
  17. The Identification of 2-(1 H -Indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d ]pyrimidine (GDC-0941) as a Potent, Selective, Orally Bioavailable Inhibitor of Class I PI3 Kinase for the Treatment of Cancer · Adrian J. Folkes · 2008 · 754 citations · Cited by this paper
  18. Implementation and outcomes of China’s drug patent linkage system: lessons from international experience · 2025 · Related
  19. Suppression of insulin feedback enhances the efficacy of PI3K inhibitors · Benjamin David Hopkins · 2018 · 732 citations · Cited by this paper
  20. An updated patent review of acetylcholinesterase inhibitors for the treatment of Alzheimer’s disease (2021–present) · 2025 · Related
  21. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study · George M. Burslem · 2017 · 700 citations · Cited by this paper
  22. Buparlisib plus fulvestrant versus placebo plus fulvestrant in postmenopausal, hormone receptor-positive, HER2-negative, advanced breast cancer (BELLE-2): a randomised, double-blind, placebo-controlled, phase 3 trial · José Baselga · 2017 · 548 citations · Cited by this paper
  23. Characterization of the Novel and Specific PI3Kα Inhibitor NVP-BYL719 and Development of the Patient Stratification Strategy for Clinical Trials · Christine M. Fritsch · 2014 · 510 citations · Cited by this paper
  24. Mutation of the PIK3CA oncogene in human cancers · Bedri Karakas · 2006 · 505 citations · Cited by this paper
  25. Helical domain and kinase domain mutations in p110α of phosphatidylinositol 3-kinase induce gain of function by different mechanisms · Li Zhao · 2008 · 444 citations · Cited by this paper
  26. Mechanism of Two Classes of Cancer Mutations in the Phosphoinositide 3-Kinase Catalytic Subunit · Nabil Miled · 2007 · 419 citations · Cited by this paper
  27. Classes of phosphoinositide 3-kinases at a glance · Steve Jean · 2014 · 385 citations · Cited by this paper
  28. The phase 3 DUO trial: duvelisib vs ofatumumab in relapsed and refractory CLL/SLL · Ian W. Flinn · 2018 · 345 citations · Cited by this paper
  29. Pictilisib for oestrogen receptor-positive, aromatase inhibitor-resistant, advanced or metastatic breast cancer (FERGI): a randomised, double-blind, placebo-controlled, phase 2 trial · Ian E. Krop · 2016 · 300 citations · Cited by this paper
  30. Identification of NVP-BKM120 as a Potent, Selective, Orally Bioavailable Class I PI3 Kinase Inhibitor for Treating Cancer · Matthew T. Burger · 2011 · 255 citations · Cited by this paper
  31. Time course and management of key adverse events during the randomized phase III SOLAR-1 study of PI3K inhibitor alpelisib plus fulvestrant in patients with HR-positive advanced breast cancer · Hope S. Rugo · 2020 · 196 citations · Cited by this paper
  32. Deconvolution of Buparlisib’s mechanism of action defines specific PI3K and tubulin inhibitors for therapeutic intervention · Thomas Bohnacker · 2017 · 120 citations · Cited by this paper
  33. Insulin-Driven PI3K-AKT Signaling in the Hepatocyte Is Mediated by Redundant PI3Kα and PI3Kβ Activities and Is Promoted by RAS · Angela Molinaro · 2019 · 108 citations · Cited by this paper
  34. Overall Survival with Inavolisib in PIK3CA -Mutated Advanced Breast Cancer · Komal L. Jhaveri · 2025 · 102 citations · Cited by this paper
  35. Discovery and Clinical Proof-of-Concept of RLY-2608, a First-in-Class Mutant-Selective Allosteric PI3Kα Inhibitor That Decouples Antitumor Activity from Hyperinsulinemia · Andreas S. Varkaris · 2023 · 99 citations · Cited by this paper
  36. STX-478, a Mutant-Selective, Allosteric PI3Kα Inhibitor Spares Metabolic Dysfunction and Improves Therapeutic Response in PI3Kα-Mutant Xenografts · Leonard Buckbinder · 2023 · 75 citations · Cited by this paper
  37. Phosphoinositide 3-Kinase (PI3K) Inhibitors and Breast Cancer: An Overview of Current Achievements · Alexandre Bertucci · 2023 · 43 citations · Cited by this paper
  38. Exploring a Non-ATP Pocket for Potential Allosteric Modulation of PI3Kα · Paraskevi Gkeka · 2014 · 38 citations · Cited by this paper
  39. Triggering PIK3CA Mutations in PI3K/Akt/mTOR Axis: Exploration of Newer Inhibitors and Rational Preventive Strategies · Vivek Asati · 2016 · 29 citations · Cited by this paper

Source: OpenAlex (CC0)