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lapatinib

Trade name: tykerb

Small moleculeapprovedFast Track FDA

Approved

Mar 13, 2007

Lapatinib is a small molecule and a member of the 4-anilinoquinazoline class of kinase inhibitors. It is present as the monohydrate of the ditosylate salt (trade name TYKERB). Lapatinib is dual inhibitor of the EGFR (epidermal growth factor receptor; also called HER1 or ErbB1) and HER2 receptor tyrosine kinases. Lapatinib was developed by GlaxoSmithKline, however, Novartis subsequently acquired all the rights to the drug from GlaxoSmithKline. TYKERB is indicated in combination therapy for the treatment of metastatic breast cancer that overexpresses the HER2 receptor. — NCATS

Clinical trial activity

789 trials · 299 clinical orgs · 5 marketing orgs

Phase 1
156
Phase 2
615
Phase 3
107
Phase 4
14

Earliest trial started Sep 1, 2002 (NCT00044343)

Timeline

2000s

  1. Dec 6, 2000

    SmithKline Beecham — IND Organization

  2. Dec 6, 2000

    SmithKline Beecham — IND Organization

  3. Jan 1, 2002

    GlaxoSmithKline — Earliest Phase 2 Sponsor(trial)

  4. Jan 1, 2003

    GlaxoSmithKline — Earliest Phase 1 Sponsor(trial)

  5. Jan 1, 2003

    Novartis — Earliest Phase 3 Sponsor(trial)

  6. Mar 13, 2007

    GlaxoSmithKline — Earliest FDA Approval

  7. Mar 13, 2007

    GlaxoSmithKline — NDA Organization

  8. Mar 13, 2007

    Novartis — NDA Secondary Org

  9. Mar 13, 2007

    Novartis — Marketing Organization

2010s

  1. Sep 18, 2015

    Natco Pharma — Marketing Organization

2020s

  1. Aug 16, 2024

    Teva — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewFast trackMar 13, 2007

Chemistry & pharmacology

Loading structure…

SMILES

N#CC1(c2ccc(NC(=O)c3cccnc3NCc3ccncc3)cc2)CCCC1
Mol. weight
397.48 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • apatinib
  • apatinib
  • apatinib
  • apatinib
  • apatinib
  • apatinib mesylate
  • apatinib mesylate
  • cipatinib
  • fmm
  • fmm
  • gw-2016
  • gw-2016
  • gw282974x
  • gw 282974x
  • gw-282974x
  • gw572016
  • gw572016
  • gw572016
  • gw 572016
  • gw 572016
  • gw 572016
  • gw-572016
  • gw-572016
  • gw-572016
  • gw572016f
  • gw572016f
  • gw572016f
  • gw 572016x
  • lapatanib
  • lapatinib
  • lapatinib
  • lapatinib
  • lapatinib
  • lapatinib
  • lapatinib
  • lapatinib
  • lapatinib
  • lapatinib
  • lapatinib
  • lapatinib
  • lapatinib ditosilate
  • lapatinib ditosilate hydrate
  • lapatinib ditosylate
  • lapatinib ditosylate
  • lapatinib ditosylate
  • lapatinib ditosylate
  • lapatinib ditosylate
  • lapatinib ditosylate hydrate
  • lapatinib ditosylate monohydrate
  • lapatinib ditosylate monohydrate
  • lapatinib tosilate
  • lapatinib tosilate hydrate
  • lapatinib tosilate hydrate
  • lapatinib tosilate hydrate
  • lapatinib tosilate hydrate
  • lapatinib tosilate hydrate
  • n-(3-chloro-4-(((3-fluorobenzyl)oxy)phenyl)-6-(5-(((2-methylsulfonyl)ethyl)amino)methyl) -2-furyl)-4-quinazolinamine
  • n-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine
  • n-{3-chloro-4-[(3-fluorobenzyl)oxy]phenyl}-6-[5-({[2-(methylsulfonyl)ethyl]amino}methyl)-2-furyl]-4-quinazolinamine
  • n-(3-chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine
  • n-(3-chloro-4-((3-fluorophenyl)methoxy)phenyl)-6-(5-(((2-(methylsulfonyl)ethyl)amino)methyl)-2-furanyl)-4-quinazolinamine
  • tykerb
  • tykerb
  • tykerb
  • tykerb
  • tykerb
  • tyverb
  • tyverb
  • tyverb
  • yn968d1
  • yn968d1
  • yn-968d1
  • yn-968d1

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07311408Phase 2Jan 1, 2026China Medical University
NCT07309419Phase 2/Phase 3 (Phase 3)Dec 22, 2025Fudan University
NCT07236528Phase 2Nov 30, 2025Nanjing University
NCT07267806Phase 3Oct 31, 2025Sun Yat-Sen University
NCT07192848Phase 2Sep 30, 2025Chinese Academy of Medical Sciences
NCT07105748Phase 2Aug 15, 2025Fudan University
NCT07135544Phase 2Aug 14, 2025Huazhong University of Science and Technology
NCT06973330Phase 2Jul 31, 2025Anhui Medical University
NCT07031154Phase 2Jun 30, 2025Xiamen University
NCT07033819Phase 2Jun 25, 2025Chinese Academy of Medical Sciences
NCT07026149Phase 2Jun 8, 2025Jiao Tong University
NCT06893887N/AMay 22, 2025Nanjing Tianyinshan Hospital
NCT06769425Phase 1May 7, 2025Jiangsu Hansoh Pharmaceutical Co., Ltd.
NCT06881017Phase 2May 1, 2025China Medical University
NCT06925243Phase 3Apr 15, 2025LanZhou University
NCT06913777Phase 3Apr 8, 2025Fudan University
NCT06771154Phase 2Apr 1, 2025Chinese Academy of Medical Sciences
NCT06796803Phase 2/Phase 3 (Phase 3)Feb 20, 2025Fudan University, Hengrui Therapeutics, Inc.
NCT07157969Phase 2Feb 19, 2025Chinese Academy of Medical Sciences
NCT06831175Phase 2Feb 15, 2025Sichuan University
Showing 20 of 789 trials
Page 1 / 40

Organizations

Research & Development (299)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Hengrui Therapeutics, Inc.For profit1174552010
GlaxoSmithKlineFor profit1105452002
Sun Yat-Sen UniversityAcademic/Hospital575342010
Chinese Academy of Medical SciencesAcademic/Hospital504032011
National Cancer Institute (NCI)Government503042004
Fudan UniversityAcademic/Hospital473952007
NovartisFor profit312242003
Peking UniversityAcademic/Hospital292742015
Jiao Tong UniversityAcademic/Hospital272242016
People's Liberation Army of ChinaGovernment251952010
Tianjin Medical UniversityAcademic/Hospital241552014
Fujian Medical UniversityAcademic/Hospital211842016
Henan Medical UniversityAcademic/Hospital161622017
Nanjing Medical UniversityAcademic/Hospital161442014
Hebei UniversityAcademic/Hospital151432015
Huazhong University of Science and TechnologyAcademic/Hospital141132015
Capital Medical UniversityAcademic/Hospital131342015
Zhejiang UniversityAcademic/Hospital131232015
Sichuan UniversityAcademic/Hospital10822016
University of Texas at HoustonAcademic/Hospital10732007
299 organizations
Page 1 / 15

Marketing (6)

OrganizationOrg typeRelationshipDate
GlaxoSmithKlineFor profitNDAMar 13, 2007
Natco PharmaFor profitMKTGSep 18, 2015
NovartisFor profitNDA2Mar 13, 2007
NovartisFor profitMKTGMar 13, 2007
SmithKline BeechamFor profitINDDec 6, 2000
TevaFor profitMKTGAug 16, 2024