Tirofiban

Summary

Tirofiban (CHEMBL916) is an approved small-molecule fibrin modulating drug (ATC B01AC17); indicated across 13 conditions including thrombotic disease and myocardial infarction.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• ATC class: B01AC17
• Indications: 13 conditions
• Clinical trials: 48
• Chemistry: 440.6 Da · C22H36N2O5S

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL916
Name	Tirofiban
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	60947
ChEBI	CHEBI:9605
ATC	B01AC17
Molecular formula	C22H36N2O5S
Molecular weight	440.6
InChIKey	COKMIXFXJJXBQG-NRFANRHFSA-N

SMILES: CCCCS(=O)(=O)N[C@@H](CC1=CC=C(C=C1)OCCCCC2CCNCC2)C(=O)O

IUPAC name: (2S)-2-(butylsulfonylamino)-3-[4-(4-piperidin-4-ylbutoxy)phenyl]propanoic acid

ChEBI definition: A member of the class of piperidines that is L-tyrosine in which a hydrogen attached to the amino group is replaced by a butylsulfonyl group and in which the hydrogen attached to the phenolic hydroxy group is replaced by a 4-(piperidin-4-yl)butyl group.

Pharmacological roles (ChEBI): fibrin modulating drug, platelet glycoprotein-IIb/IIIa receptor antagonist, anticoagulant.

Also known as: Agrastat, Tirofiban, tirofiban, TIROFIBAN, Tirofiban_HCL monohydrate

Parent form; salt/anhydrous children: CHEMBL1704, CHEMBL3189072

Patent coverage: 4,101 distinct patent families (16,908 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
	integrin αIIbβ3	Inhibition	9.43

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Integrin alpha-V/beta-3, Integrin alpha-IIb/beta-3, Muscarinic acetylcholine receptor M2, Sodium-dependent serotonin transporter, Integrin subunit alpha 2b/beta-3.

Bioactivity

ChEMBL activities: 38 potent at pChembl ≥ 5 of 41 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
ITGB3	9.43	IC50	0.37	nM	CHEMBL_ACT_13338438
ITGB3	9.43	IC50	0.37	nM	CHEMBL_ACT_8040743
ITGB3	9.05	ED50	0.9	nM	CHEMBL_ACT_876522
ITGB3	9.02	IC50	0.95	nM	CHEMBL_ACT_12675361
ITGB3	9.02	IC50	0.95	nM	CHEMBL_ACT_8058503
ITGB3	9.01	ED50	0.97	nM	CHEMBL_ACT_307222
ITGB3	9.01	ED50	0.97	nM	CHEMBL_ACT_819958
ITGB3	8.92	IC50	1.2	nM	CHEMBL_ACT_20706904
ITGB3	8.92	IC50	1.2	nM	CHEMBL_ACT_22992199
ITGB3	8.89	IC50	1.3	nM	CHEMBL_ACT_19132362
ITGB3	8.72	IC50	1.9	nM	CHEMBL_ACT_16533350
ITGB3	8.72	Kd	1.9	nM	CHEMBL_ACT_506243
ITGB3	8.62	IC50	2.4	nM	CHEMBL_ACT_13390153
ITGB3	8.62	IC50	2.4	nM	CHEMBL_ACT_15730697
ITGB3	8.62	IC50	2.4	nM	CHEMBL_ACT_15730706
ITGB3	8.3	IC50	5	nM	CHEMBL_ACT_457527
ITGB3	8.14	IC50	7.3	nM	CHEMBL_ACT_22451722
ITGB3	8.05	IC50	9	nM	CHEMBL_ACT_204374
ITGB3	8.05	IC50	9	nM	CHEMBL_ACT_223042
ITGB3	8.03	IC50	9.4	nM	CHEMBL_ACT_22451999
ITGB3	8	IC50	10	nM	CHEMBL_ACT_1280932
ITGB3	7.96	IC50	11	nM	CHEMBL_ACT_20604686
ITGB3	7.96	IC50	11	nM	CHEMBL_ACT_457526
ITGB3	7.96	IC50	11	nM	CHEMBL_ACT_819957
ITGB3	7.89	Kd	13	nM	CHEMBL_ACT_307223
ITGB3	7.89	Kd	13	nM	CHEMBL_ACT_506242
ITGB3	7.87	EC50	13.6	nM	CHEMBL_ACT_8058514
ITGB3	7.82	IC50	15	nM	CHEMBL_ACT_1302644
ITGB3	7.82	IC50	15	nM	CHEMBL_ACT_506241
ITGB3	7.82	Kd	15	nM	CHEMBL_ACT_819959
ITGB3	7.5	IC50	32	nM	CHEMBL_ACT_15730701
ITGB3	7.5	IC50	32	nM	CHEMBL_ACT_15730711
ITGB3	7.45	IC50	35.7	nM	CHEMBL_ACT_935329
ITGB3	7.4	IC50	40	nM	CHEMBL_ACT_16847079
ITGB3	7.05	IC50	90	nM	CHEMBL_ACT_16847101
Q8R2H2	6.89	IC50	130	nM	CHEMBL_ACT_23173837
ITGB3	6.22	IC50	600	nM	CHEMBL_ACT_14750219
SLC6A4	5	AC50	9960	nM	CHEMBL_ACT_25151346

Target pathways

No target-pathway data for this drug (no mapped target genes).

Indications & clinical

Indications

1 approved indication. FDA phase 4, plus an anticancer drug’s labelled cancer uses (which ChEMBL often logs at phase 3).

Indication	Phase	MONDO	EFO
thrombotic disease	4	MONDO:0000831	HP:0004419

11 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
myocardial infarction	3	MONDO:0005068	EFO:0000612
acute coronary syndrome	3	MONDO:0005542	EFO:0005672
coronary artery disorder	3	MONDO:0005010	EFO:0001645
acute myocardial infarction	3	MONDO:0004781	EFO:0008583
atherosclerosis	3	MONDO:0005311	EFO:0003914
venous thromboembolism	2	MONDO:0005399	EFO:0004286
viral pneumonia	2	MONDO:0006012	EFO:0007541
respiratory failure	2	MONDO:0021113	EFO:0009686
stroke disorder	2	MONDO:0005098	EFO:0000712
severe acute respiratory syndrome	2	MONDO:0005091	MONDO:0100096
kidney failure	1	MONDO:0001106	HP:0000083

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 48.

Phase distribution

Phase	Trials
PHASE4	22
PHASE3	10
PHASE2/PHASE3	5
Not specified	5
PHASE2	3
PHASE1/PHASE2	2
PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06769256	PHASE4	RECRUITING	Intracoronary rhTNK-tPA Versus Tirofiban in Patients With STEMI and High Thrombus Burden
NCT07095790	PHASE4	RECRUITING	Tirofiban With Sequential Dual Antiplatelet Therapy in Mild Stroke
NCT07290751	PHASE4	RECRUITING	Intravenous Thrombolysis Combined With Tirofiban in Acute Ischemic Stroke
NCT00229515	PHASE4	UNKNOWN	Multicentre 2x2 Factorial Randomised Study Comparing Tirofiban Versus Abciximab and SES Versus BMS in AMI
NCT00300833	PHASE4	UNKNOWN	Treating Acute MI Patients With Aggrastat on Their Way to Hospital
NCT00398463	PHASE4	COMPLETED	Study of Tirofiban Administration in Patients With Aspirin and or Clopidogrel Resistance
NCT00407771	PHASE4	UNKNOWN	The Effects of Tirofiban in Diabetic Patients Undergoing Elective Percutaneous Coronary Intervention
NCT00445263	PHASE4	TERMINATED	Comparison of Two Treatment Strategies in Patients With an Acute Coronary Syndrome Without ST Elevation
NCT00538317	PHASE4	COMPLETED	GPIIbIIIa Inhibitors in the RESCUe and RESURCOR Networks at the Acute Myocardial Infarction
NCT00566891	PHASE4	COMPLETED	Safety of High-dose Tirofiban During Coronary Angioplasty
NCT00611169	PHASE4	COMPLETED	The Effects of Facilitated Percutaeous Coronary Intervention in Acute Myocardial Infarction
NCT00790387	PHASE4	COMPLETED	Tirofiban and Enoxaparin in High Risk Coronary Intervention
NCT01498003	PHASE4	COMPLETED	Tirofiban in Stenting for Long Coronary Lesion
NCT02054000	PHASE4	COMPLETED	Intracoronary Tirofiban on No-Reflow Phenomena
NCT02131220	PHASE4	COMPLETED	Effects of Intracoronary Prourokinase on the Coronary Flow During Primary Percutaneous Coronary Intervention for Acute Myocardial Infarction
NCT02294994	PHASE4	UNKNOWN	Efficacy and Safety of Different Dose of Tirofiban in Interventional Treatment of Complex Coronary Artery Disease
NCT02978040	PHASE4	COMPLETED	Randomized Comparison of Cangrelor, Tirofiban and Prasugrel in Patients With STEMI Referred for Primary PCI.
NCT03114995	PHASE4	COMPLETED	Tailored Use of Tirofiban for Non-ST-elevation Acute Coronary Syndrome Patients
NCT03797729	PHASE4	UNKNOWN	Early Initiation of Low Dose Tirofiban for PPCI in STEMI Patients.
NCT05225961	PHASE4	COMPLETED	ATILA Project: Aspirin Versus Tirofiban in Endovascular Treatment for Patients With Acute Ischemic Stroke Due to Tandem Lesion
NCT05310968	PHASE4	COMPLETED	Study on Tirofiban With Aspirin in the Treatment of Acute Penetrating Artery Territory Infarction
NCT05841147	PHASE4	UNKNOWN	Reduction of Microembolism After the Intervention Surgery of Intracranial Aneurysms by Administration of Tirofiban
NCT05728333	PHASE2/PHASE3	RECRUITING	Intravenous Tirofiban Versus Alteplase Before Mechanical Thrombectomy in Stroke
NCT06319846	PHASE3	RECRUITING	Tirofiban for Patients With intraCranial Artery Stenosis and High-risk Acute Non-disabling Cerebrovascular Events(CHANCE-4）
NCT06373042	PHASE2/PHASE3	NOT_YET_RECRUITING	Tirofiban for Successful Endovascular Stroke Thrombectomy
NCT07111806	PHASE3	NOT_YET_RECRUITING	Intravenous Tirofiban After Delayed Thrombolysis in Stroke
NCT07335107	PHASE3	NOT_YET_RECRUITING	Intravenous Tirofiban After Bridging Therapy for Acute Stroke With Atherosclerotic Large Artery Occlusion
NCT07379190	PHASE3	NOT_YET_RECRUITING	HR-MRI-Directed Tirofiban Therapy for Late-Window Acute Ischemic Stroke (TIAN)
NCT07537933	PHASE3	NOT_YET_RECRUITING	Intra-Arterial Tirofiban After Complete Recanalization for Acute Intracranial Large-Vessel Occlusion
NCT01245725	PHASE3	WITHDRAWN	Aggrastat Truncated Length Against Standard Therapies in Percutaneous Coronary Intervention
NCT01336348	PHASE3	COMPLETED	Facilitation Through Aggrastat By drOpping or Shortening Infusion Line in Patients With ST-segment Elevation Myocardial Infarction Compared to or on Top of PRasugrel Loading dOse
NCT01598337	PHASE3	UNKNOWN	The Effect Of Antiplatelets Therapy On Saphenous Vein Coronary Artery Bypass Graft Patency
NCT01660373	PHASE3	UNKNOWN	Comparison of Antiplatelet Effect of Ticagrelor vs Tirofiban in Patients With Non-ST Elevation Acute Coronary Syndrome
NCT03357133	PHASE2/PHASE3	TERMINATED	Tirofiban for Patients Treated With Alteplase
NCT06037889	PHASE3	COMPLETED	Efficacy and Safety of Tirofiban for Patients With BAD (BRANT)
NCT06238115	PHASE2/PHASE3	COMPLETED	Tirofiban for Reduction of Thromboembolic Events in Endovascular Unruptured Aneurysm Repair
NCT06265051	PHASE2/PHASE3	COMPLETED	Tirofiban After Successful MT Recanalization in AIS
NCT07493577	PHASE1/PHASE2	NOT_YET_RECRUITING	Induced Suppression of Platelet Activity in Aneurysmal Subarachnoid Hemorrhage Management-2 (iSPASM-2)
NCT01522417	PHASE2	COMPLETED	Shortened Aggrastat® Versus Integrilin in Percutaneous Coronary Intervention
NCT03691727	PHASE1/PHASE2	COMPLETED	Induced Suppression of Platelets Activity in Aneurysmal SAH Management (iSPASM)
NCT04368377	PHASE2	COMPLETED	Enhanced Platelet Inhibition in Critically Ill Patients With COVID-19
NCT05188417	PHASE2	UNKNOWN	A Study Evaluating the Safety and Efficacy of Tirofiban in Combination With Alteplase in Acute Ischemic Stroke
NCT01766154	PHASE1	COMPLETED	Pharmacokinetic Evaluation of Tirofiban Using a Single High-Dose Bolus In Subjects With Varying Degrees of Renal Function
NCT06045156	Not specified	RECRUITING	Early Tirofiban Administration After Intravenous Thrombolysis in Acute Ischemic Stroke
NCT06966674	Not specified	RECRUITING	No-Reflow in Patients With STEMI After Intracoronary Tirofiban After Opening of the Track
NCT07026318	Not specified	RECRUITING	Endovascular Therapy Combined With Tirofiban for Intracranial Atherosclerotic Acute Ischemic Stroke
NCT00713557	Not specified	TERMINATED	Shanghai Registry of Acute Coronary Events
NCT03048019	Not specified	TERMINATED	Antiplatelet Effects of Tirofiban vs. Cangrelor N-STEMI Patients Undergoing Percutaneous Coronary Intervention

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).