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neratinib maleate

Trade name: nerlynx

Small moleculeapproved

Approved

Jul 17, 2017

Neratinib (HKI-272) is a pan-HER inhibitor, this irreversible tyrosine kinase inhibitor binds and inhibits the tyrosine kinase activity of epidermal growth factor receptors, EGFR (or HER1), HER2 and HER4, which leads to reduced phosphorylation and activation of downstream signaling pathways. Neratinib is a modified form of the discontinued compound pelitinib, and was originally being develoAdditionally, phase II development of oral neratinib as a neoadjuvant therapy for breast cancer, as a second-line therapy for non-small cell lung cancer, and for other solid tumours is also in progress in numerous countries worldwide. ped by Wyeth (later Pfizer). Oral neratinib is awaiting approval as an extended adjuvant therapy for breast cancer in the EU and in the US. Blocking HER2 function by a small molecule kinase inhibitor, such as neratinib, represents an attractive alternate strategy for the growth inhibition of HER2-positive tumours. — NCATS

Clinical trial activity

82 trials · 68 clinical orgs · 3 marketing orgs

Phase 1
37
Phase 2
55
Phase 3
4
Phase 4
0

Earliest trial started Nov 1, 2003 (NCT00146172)

Timeline

2000s

  1. Jan 1, 2003

    Puma Biotechnology, Inc. — Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2005

    Puma Biotechnology, Inc. — Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 2009

    Puma Biotechnology, Inc. — Earliest Phase 3 Sponsor(trial)

2010s

  1. Jul 17, 2017

    Puma Biotechnology, Inc. — Earliest FDA Approval

  2. Jul 17, 2017

    Puma Biotechnology, Inc. — NDA Secondary Org

  3. Jul 17, 2017

    Puma Biotechnology, Inc. — NDA Organization

2020s

  1. Jul 5, 2022

    Sandoz — Marketing Organization

  2. Jul 5, 2022

    Novartis — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedJul 17, 2017

Chemistry & pharmacology

Loading structure…

SMILES

CCOc1cc2ncc(C#N)c(Nc3ccc(OCc4ccccn4)c(Cl)c3)c2cc1NC(=O)/C=C/CN(C)C.O=C(O)/C=C\C(=O)O
Mol. weight
673.13 g/mol
Lipinski Ro5
2 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • cdp-820
  • cdp-820
  • hki272
  • hki 272
  • hki-272
  • hki-272
  • hki-272
  • hki-272
  • n-(4-(3-chloro-4-(2-pyridinylmethoxy)anilino)-3-cyano-7-ethoxy-6-quinolyl)-4-(dimethylamino)-2-butenamide
  • neratinib
  • neratinib
  • neratinib
  • neratinib
  • neratinib
  • neratinib
  • neratinib
  • neratinib maleate
  • nerlynx
  • nerlynx
  • nerlynx
  • way-179272
  • way-179272

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07152782Phase 2Nov 30, 2025Fudan University
NCT06813079Phase 2Feb 17, 2025University of Toronto
NCT05919108Phase 2Jan 31, 2025National Cancer Institute (NCI), Puma Biotechnology, Inc., Vanderbilt University
NCT06519110Phase 2Aug 10, 2024China Pharmaceutical University, Convalife
NCT05615818Phase 3Jul 18, 2024Accord Research, Belgian Group of Digestive Oncology, Cancer Research UK, Center Eugene Marquis, Institut Mutualiste Montsouris, National Cancer Institute, France, Otsuka, Pierre Fabre, Servier, UNICANCER, Université catholique de Louvain, University of London, Zymeworks Inc.
NCT06374888Phase 2Apr 30, 2024Convalife
NCT06126276Phase 2Feb 20, 2024National Cancer Institute (NCI), NRG Oncology
NCT06109467Phase 2Jan 12, 2024National Comprehensive Cancer Network, Puma Biotechnology, Inc., University of South Florida
NCT06008275Early Phase 1 (Phase 1)Nov 30, 2023Baylor Scott and White, Baylor University
NCT06029816Phase 2Nov 20, 2023Convalife, Sun Yat-Sen University
NCT05933395Phase 2Oct 10, 2023Dartmouth University
NCT06015113N/ASep 30, 2023Xi'an International Medical Center Hospital
NCT05760612Phase 3Feb 16, 2023Sun Yat-Sen University
NCT05388149Phase 2Dec 6, 2022University of Toronto
NCT05252988Phase 2Aug 31, 2022Hospital General Universitario Gregorio Marañon, Pierre Fabre, Puma Biotechnology, Inc., Spanish Breast Cancer Research Group
NCT05243641Phase 1/Phase 2 (Phase 2)Aug 18, 2022Celcuity, Novartis, Puma Biotechnology, Inc., University of Texas at Houston
NCT05274048Phase 1Jun 24, 2022National Comprehensive Cancer Network, Puma Biotechnology, Inc., Temple University
NCT05372614Phase 1Jun 17, 2022National Cancer Institute (NCI), Yale University
NCT05154396Phase 2Jan 1, 2022Chinese Academy of Medical Sciences
NCT04901299Phase 2Dec 31, 2021Celcuity, Harvard University, Puma Biotechnology, Inc.
Showing 20 of 82 trials
Page 1 / 5

Organizations

Research & Development (68)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Puma Biotechnology, Inc.For profit543432003
Harvard UniversityAcademic/Hospital5512012
NSABP FoundationAcademic/Hospital5522010
National Cancer Institute (NCI)Government4222016
University of Texas at HoustonAcademic/Hospital4322016
CelcuityFor profit3012019
ConvalifeFor profit3312023
Sun Yat-Sen UniversityAcademic/Hospital3122021
University of California, San FranciscoAcademic/Hospital3222010
National Comprehensive Cancer NetworkAcademic/Hospital2022022
PfizerFor profit2012011
Pierre FabreFor profit2022022
University of LondonAcademic/Hospital2122016
University of RochesterAcademic/Hospital2112021
University of TorontoAcademic/Hospital2212022
Virginia Commonwealth UniversityAcademic/Hospital2222019
Accelerate Brain Cancer CureAcademic/Hospital1012017
Accord ResearchFor profit1012024
Baylor Scott and WhiteAcademic/Hospital1012023
Baylor UniversityAcademic/Hospital1112023
68 organizations
Page 1 / 4

Marketing (4)

OrganizationOrg typeRelationshipDate
NovartisFor profitMKTGJul 5, 2022
Puma Biotechnology, Inc.For profitNDA2Jul 17, 2017
Puma Biotechnology, Inc.For profitNDAJul 17, 2017
SandozFor profitMKTGJul 5, 2022