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tirofiban

Trade name: aggrastat

Small moleculeapproved

Approved

May 14, 1998

Tirofiban is a non-peptide antagonist of the platelet glycoprotein (GP) IIb/IIIa receptor. Tirofiban is a reversible, competitive inhibitor of GP IIb/IIIa receptors, exerting its effects via the prevention of the binding of fibrinogen and other ligands, resulting in the inhibition of the last common step of thrombi formation. Tirofiban was discovered by Merck, USA, and was approved by the FDA in 1998 under the trade name AGGRASTAT. AGGRASTAT, in combination with heparin, is indicated for the treatment of acute coronary syndrome, including patients who are to be managed medically and those undergoing percutaneous transluminal coronary angioplasty or atherectomy. AGGRASTAT reduces the risk of ischaemic complications in patients with unstable angina/non-Q-wave myocardial infarction and high-risk patients undergoing revascularisation when used against a background of heparin and aspirin. Furthermore, the drug has an acceptable tolerability profile. Therefore, intravenous tirofiban is likely to be used as an adjunct to heparin and aspirin in patients with acute coronary syndromes including high-risk patients undergoing revascularisation. — NCATS

Clinical trial activity

58 trials · 94 clinical orgs · 6 marketing orgs

Phase 1
5
Phase 2
16
Phase 3
19
Phase 4
25

Earliest trial started Nov 1, 1999 (NCT00251576)

Timeline

1990s

  1. May 14, 1998

    Merck — Earliest FDA Approval

  2. May 14, 1998

    Medicure — NDA Secondary Org

  3. May 14, 1998

    Merck — NDA Organization

  4. Jan 1, 1999

    Merck — Earliest Phase 3 Sponsor(trial)

2010s

  1. Jan 1, 2012

    Medicure — Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2013

    Medicure — Earliest Phase 1 Sponsor(trial)

  3. Jan 31, 2017

    Gland Pharma Ltd — Marketing Organization

2020s

  1. Apr 8, 2021

    Fosun — Marketing Organization

  2. Apr 21, 2022

    Eugia Pharma — Marketing Organization

  3. Feb 7, 2023

    Nexus Pharmaceuticals — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewMay 14, 1998

Chemistry & pharmacology

Loading structure…

SMILES

CCCCS(=O)(=O)N[C@@H](Cc1ccc(OCCCCC2CCNCC2)cc1)C(=O)O.Cl.O
Mol. weight
495.08 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Delivery
Parenteral
Availability
Prescription Only

Oral

No

Parenteral

Yes

Topical

No

Sources

Also known as

  • (2s)-2-(butylsulfonylamino)-3-[4-(4-piperidin-4-ylbutoxy)phenyl]propanoic acid
  • (2s)-2-(butylsulfonylamino)-3-[4-(4-piperidin-4-ylbutoxy)phenyl]propanoic acid
  • aggrastat
  • aggrastat
  • aggrastat
  • aggrastat
  • aggrastat
  • aggrestat
  • agrastat
  • cahill may roberts brand of tirofiban hydrochloride monohydrate
  • l 700462
  • l-700462
  • l-700462
  • l-700462
  • l-700,462
  • l-700,462
  • merck brand of tirofiban hydrochloride monohydrate
  • merck frosst brand of tirofiban hydrochloride monohydrate
  • merck sharp & dohme brand of tirofiban hydrochloride monohydrate
  • mk 383
  • mk-383
  • mk-383
  • mk-383
  • msd brand of tirofiban hydrochloride monohydrate
  • n-(butylsulfonyl)-o-(4-(4-piperidyl)butyl)-l-tyrosine
  • n-(butylsulfonyl)-o-(4-(4-piperidyl)butyl)-l-tyrosine
  • n-(butylsulfonyl)-o-(4-(4-piperidyl)butyl)-l-tyrosine
  • tirofiban
  • tirofiban
  • tirofiban
  • tirofiban
  • tirofiban
  • tirofiban
  • tirofiban
  • tirofiban
  • tirofiban
  • tirofiban
  • tirofiban hcl
  • tirofiban hcl
  • tirofiban hcl
  • tirofiban hydrochloride
  • tirofiban hydrochloride
  • tirofiban hydrochloride
  • tirofiban hydrochloride
  • tirofiban hydrochloride
  • tirofiban hydrochloride monohydrate
  • tirofiban hydrochloride monohydrate
  • tirofibanum
  • tirofibanum

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07290751Phase 4Dec 10, 2025Capital Medical University
NCT07111806Phase 3Dec 1, 2025Sun Yat-Sen University
NCT07135089Phase 3Oct 1, 2025People's Liberation Army of China
NCT07095790Phase 4Aug 30, 2025Soochow University
NCT07026318N/AAug 15, 2025Capital Medical University
NCT06966674N/AMay 12, 2025Kafrelsheikh University
NCT06702657N/AFeb 15, 2025Changhai Hospital, The First People's Hospital of Changzhou
NCT06769256Phase 4Jan 1, 2025Henan Institute of Cardiovascular Epidemiology
NCT06587347Phase 2/Phase 3 (Phase 3)Nov 20, 2024Capital Medical University
NCT06373042Phase 2/Phase 3 (Phase 3)Jul 31, 2024Chongqing Medical University, Government of China, Mianyang Central Hospital, People's Liberation Army of China
NCT06319846Phase 3Jul 11, 2024Capital Medical University
NCT06265051Phase 2/Phase 3 (Phase 3)Apr 9, 2024Capital Medical University, Chengde Medical University, Enshi Tujia and Miao Autonomous Prefecture Central Hospital, Hanyang University, Huangshi Central Hospital, Huazhong University of Science and Technology, Jingzhou Central Hospital, Nanjing University, Nanyang Central Hospital, People's Hospital Of Yichang, Shiyan Taihe Hospital, Soochow University, Wuhan Central Hospital, Wuhan Puren Hospital, Wuhan University, Xiamen University, Xiang Yang NO.1 People's Hospital, Xianning Central Hospital, Zhengzhou University
NCT06238115Phase 2/Phase 3 (Phase 3)Mar 4, 2024Capital Medical University
NCT06045156N/AJan 1, 2024Jinlin University
NCT06134622Phase 3Jan 1, 2024University of Science and Technology of China
NCT06037889Phase 3Nov 9, 2023Chinese Academy of Medical Sciences
NCT05841147Phase 4Apr 25, 2023Nanjing Medical University
NCT05604638Phase 4Mar 31, 2023Guangxi Medical University, Shijiazhuang Pharma Group (CSPC)
NCT05728333Phase 2/Phase 3 (Phase 3)Mar 1, 2023Government of China, People's Liberation Army of China, Zhejiang University
NCT05310968Phase 4Nov 30, 2022Capital Medical University, Grand Pharma (China) Co., Ltd
Showing 20 of 58 trials
Page 1 / 3

Organizations

Research & Development (94)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Capital Medical UniversityAcademic/Hospital9832017
People's Liberation Army of ChinaGovernment5322018
MedicureFor profit3332010
MerckFor profit3121999
Nanyang Central HospitalAcademic/Hospital3022018
University of FerraraAcademic/Hospital3322004
Zhengzhou UniversityAcademic/Hospital3222018
Anyang Regional HospitalAcademic/Hospital2012018
Fudan UniversityAcademic/Hospital2212015
Government of ChinaGovernment2012023
Henan Medical UniversityAcademic/Hospital2012018
Henan University of Traditional Chinese MedicineAcademic/Hospital2012018
Huazhong University of Science and TechnologyAcademic/Hospital2212021
Jiao Tong UniversityAcademic/Hospital2122011
Jincheng People’s HospitalAcademic/Hospital2012018
Kaifeng Central HospitalAcademic/Hospital2012018
Lushan People’s HospitalAcademic/Hospital2012018
Nanjing Medical UniversityAcademic/Hospital2222016
Puyang Oil Field General HospitalAcademic/Hospital2012018
Puyang People's HospitalAcademic/Hospital2012018
94 organizations
Page 1 / 5

Marketing (9)

OrganizationOrg typeRelationshipDate
Eugia PharmaFor profitMKTGApr 21, 2022
Eugia PharmaFor profitSYNMay 1, 2023
FosunFor profitMKTGApr 8, 2021
Gland Pharma LtdFor profitMKTGJan 31, 2017
Gland Pharma LtdFor profitSYNApr 8, 2021
MedicureFor profitNDA2May 14, 1998
MerckFor profitNDAMay 14, 1998
Nexus PharmaceuticalsFor profitMKTGFeb 7, 2023
Nexus PharmaceuticalsFor profitSYNFeb 7, 2023