ITGB3 integrin subunit beta 3
ENSG00000259207 · protein coding · Open Targets profile
Integrin alpha-V/beta-3 (ITGAV:ITGB3) is a receptor for cytotactin, fibronectin, laminin, matrix metalloproteinase-2, osteopontin, osteomodulin, prothrombin, thrombospondin, vitronectin and von Willebrand factor (VWF). Integrin alpha-IIb/beta-3 (ITGA2B:ITGB3) is a receptor for fibronectin, fibrinogen, plasminogen, prothrombin, thrombospondin and vitronectin. Integrins alpha-IIb/beta-3 and alpha- V/beta-3 recognize the sequence R-G-D in a wide array of ligands. Integrin alpha-IIb/beta-3 recognizes the sequence H-H-L-G-G-G-A-K-Q-A- G-D-V in fibrinogen gamma chain (By similarity). Following activation integrin alpha-IIb/beta-3 brings about platelet/platelet interaction through binding of soluble fibrinogen (PubMed:9111081). This step leads to rapid platelet aggregation which physically plugs ruptured endothelial surface. Fibrinogen binding enhances SELP expression in activated platelets (By similarity). ITGAV:ITGB3 binds to fractalkine (CX3CL1) and acts as its coreceptor in CX3CR1-dependent fractalkine signaling (PubMed:23125415, PubMed:24789099). ITGAV:ITGB3 binds to NRG1 (via EGF domain) and this binding is essential for NRG1-ERBB signaling (PubMed:20682778). ITGAV:ITGB3 binds to FGF1 and this binding is essential for FGF1 signaling (PubMed:18441324). ITGAV:ITGB3 binds to FGF2 and this binding is essential for FGF2 signaling (PubMed:28302677). ITGAV:ITGB3 binds to IGF1 and this binding is essential for IGF1 signaling (PubMed:19578119). ITGAV:ITGB3 binds to IGF2 and this binding is essential for IGF2 signaling (PubMed:28873464). ITGAV:ITGB3 binds to IL1B and this binding is essential for IL1B signaling (PubMed:29030430). ITGAV:ITGB3 binds to PLA2G2A via a site (site 2) which is distinct from the classical ligand-binding site (site 1) and this induces integrin conformational changes and enhanced ligand binding to site 1 (PubMed:18635536, PubMed:25398877). ITGAV:ITGB3 acts as a receptor for fibrillin-1 (FBN1) and mediates R-G-D-dependent cell adhesion to FBN1 (PubMed:12807887). In brain, plays a role in synaptic transmission and plasticity. Involved in the regulation of the serotonin neurotransmission, is required to localize to specific compartments within the synapse the serotonin receptor SLC6A4 and for an appropriate reuptake of serotonin. Controls excitatory synaptic strength by regulating GRIA2-containing AMPAR endocytosis, which affects AMPAR abundance and composition (By similarity). ITGAV:ITGB3 act as a receptor for CD40LG (PubMed:31331973). ITGAV:ITGB3 acts as a receptor for IBSP and promotes cell adhesion and migration to IBSP (PubMed:10640428). Integrin ITGA2B:ITGB3 is also the receptor of the erythrocyte-specific ICAM4 ligand involved in heterotypic cell-cell adhesion between erythrocytes and activated platelets (PubMed:12477717). ITGAV:ITGB3 acts as a receptor for SNED1 and mediates R-G-D-dependent cell adhesion to SNED1 (PubMed:39713860). {ECO:0000250|UniProtKB:O54890, ECO:0000269|PubMed:10640428, ECO:0000269|PubMed:12477717, ECO:0000269|PubMed:12807887, ECO:0000269|PubMed:18441324, ECO:0000269|PubMed:18635536, ECO:0000269|PubMed:19578119, ECO:0000269|PubMed:20682778, ECO:0000269|PubMed:23125415, ECO:0000269|PubMed:24789099, ECO:0000269|PubMed:25398877, ECO:0000269|PubMed:28302677, ECO:0000269|PubMed:28873464, ECO:0000269|PubMed:29030430, ECO:0000269|PubMed:31331973, ECO:0000269|PubMed:39713860, ECO:0000269|PubMed:9111081, ECO:0000269|PubMed:9195946, ECO:0000303|PubMed:16322781, ECO:0000303|PubMed:17635696}.
Each band is a group of drugs. It runs from the kind of drug on the left to the furthest stage that drug has reached in any disease on the right. Thicker bands mean more drugs.
Approved bands are highlighted. Withdrawn means the drug was pulled from the market or from development. A combined phase counts as the later one (Phase 1/2 is shown as Phase 2). Hover a band for the drug names. Source: Open Targets Platform, fetched live.
Each row is a cancer, strongest overall evidence first. The two dots show how strong the inherited (germline) and tumour-mutation (somatic) evidence is; the line between them is the gap.
Scores run from 0 (no evidence) to 1 (strongest). A missing dot at 0 means Open Targets holds no evidence of that kind. Source: Open Targets Platform, fetched live.
Tractability
- Small molecule
- Approved Drug, Structure with Ligand, High-Quality Ligand, Druggable Family
- Antibody
- Approved Drug, UniProt loc high conf, GO CC high conf, UniProt loc med conf, UniProt SigP or TMHMM, Human Protein Atlas loc
- PROTAC
- Database Ubiquitination, Small Molecule Binder
- Other modalities
- Approved Drug
gnomAD loss of function constraint: o/e 0.559249997138977 (upper bound 0.7113500237464905). Low values mean loss of function is poorly tolerated, a safety flag for inhibition.
Who runs trials of these drugs
Principal investigators and study chairs on 38 registry trials, updated in the last three years, of the most advanced drugs against ITGB3 (tirofiban, abciximab, zalunfiban, cilengitide, ATN-161, intetumumab, etaracizumab, tadocizumab, abituzumab), ranked by Phase 2+ trials. Live from ClinicalTrials.gov.
- zhongming qiuXinqiao Hospital of the Army Medical University · 4 of 4 trials Phase 2+Ph2/Ph3NCT07842185 · A Multicenter, Open-label, Randomized, Non-inferiority Clinical Trial With Blinded Endpoint Assessment of Early Tirofiban After Intravenous Thrombolysis in Acute Ischemic Strokebrief
- Arnoud WJ Van 't HofMaastricht University Medical Center · 1 of 1 trials Phase 2+
- Brian Mac GroryDuke University · 1 of 1 trials Phase 2+
- Congguo YinHangzhou First Hospital of Westlake University · 1 of 1 trials Phase 2+
- Elena Zapata-ArrizadaVirgen del Rocío Hospital, Seville, Spain · 1 of 1 trials Phase 2+
- Emad HasanDuke University · 1 of 1 trials Phase 2+
- Gang LiShanghai East Hospital · 1 of 1 trials Phase 2+
- Hyun-Jae KangAssistant professor, Cardiology, Department of internal medicine,Seoul National University Hospital · 1 of 1 trials Phase 2+
- Jijun ShiSecond Affiliated Hospital of Soochow University · 1 of 1 trials Phase 2+
- Jing JingBeijing Tiantan Hospital · 1 of 1 trials Phase 2+
- Jun NiThe office for BRANT study · 1 of 1 trials Phase 2+
- Qinjian SunShandong Provincial Hospital · 1 of 1 trials Phase 2+
- Yamei TangSun Yat-Sen Memorial Hospital of Sun Yat-Sen University · 1 of 1 trials Phase 2+
- Yilong WangBeijing Tiantan Hospital, Capital Medical University, Beijing, China · 1 of 1 trials Phase 2+
- Cheol Woong YuCardiovascular center, Korea University Anam Hospital · 0 of 1 trials Phase 2+
Registry trials of tirofiban, abciximab, zalunfiban, cilengitide, ATN-161, intetumumab, etaracizumab, tadocizumab, abituzumab updated in the last three years, counted by the country group of their listed sites. A trial with sites in several groups counts in each; 33 of 34 have all sites in one country.
Site counts are not patients per country, and trials registered only outside ClinicalTrials.gov are not covered. Where sites are is a fact about the record, not a judgement of its quality. Europe is the EU and EEA, the UK and Switzerland. 4 trials list no sites and are left out. Source: ClinicalTrials.gov, fetched live.
27 trials of drugs against ITGB3 were stopped early; 9 give no reason
Terminated, withdrawn and suspended interventional trials of tirofiban, abciximab, zalunfiban, cilengitide, ATN-161, intetumumab, etaracizumab, tadocizumab, abituzumab, newest update first, live from ClinicalTrials.gov. Each reason is quoted exactly as the registry gives it; we do not sort reasons into safety, efficacy or business. Dates are the last registry update. Showing the 25 most recent of 27.
- terminated · 2026-04-27 · Seoul National University Hospital · glycoprotein IIb/IIIa inhibitor (abciximab)“The study was terminated early due to a shortage of research and analytical personnel, which prevented the completion of the study as planned”
- withdrawn · 2022-09-21 · University of Iowa · Tirofiban Hydrochloride“PI has left the Institution”
- terminated · 2020-09-09 · Capital Medical University · Tirofiban“The number and speed of enrollment were significantly less than expected.”
- withdrawn · 2020-03-18 · SFJ Pharmaceuticals X, LTD. · abituzumab“Co-development decision”
- terminated · 2019-06-18 · EMD Serono Research & Development Institute, Inc. · Abituzumab 1500 mg, Abituzumab 500 mg“Difficulties experienced in identifying participants who meet the eligibility criteria of the trial.”
- withdrawn · 2018-03-13 · Medicure · Tirofiban (Aggrastat)“Study was not initiated, change in clinical development”
- withdrawn · 2018-01-19 · M.D. Anderson Cancer Center · CilengitideNo reason given
- terminated · 2017-06-14 · National Cancer Institute (NCI) · cilengitide“due to poor accrual”
- withdrawn · 2015-12-18 · University of Rochester · AbciximabNo reason given
- terminated · 2015-07-21 · Martin-Luther-Universität Halle-Wittenberg · Cilengitide“due to an altered benefit/risk assessment.”
- terminated · 2015-04-28 · National Cancer Institute (NCI) · CilengitideNo reason given
- withdrawn · 2015-03-26 · St. Louis University · Abciximab“Insufficient recruitment”
- terminated · 2015-02-27 · Hospital Avicenne · TIROFIBAN“Because of inclusion delay”
- terminated · 2014-05-15 · National Cancer Institute (NCI) · etaracizumabNo reason given
- terminated · 2014-04-25 · SOS Attaque Cérébrale · matched by the registry's drug synonymsNo reason given
- terminated · 2014-02-04 · Merck KGaA, Darmstadt, Germany · matched by the registry's drug synonyms“Discontinuation of development program”
- terminated · 2013-06-05 · National Cancer Institute (NCI) · cilengitideNo reason given
- terminated · 2013-06-03 · National Cancer Institute (NCI) · cilengitide“Administratively complete.”
- terminated · 2013-01-24 · National Cancer Institute (NCI) · cilengitide“Administratively complete.”
- terminated · 2013-01-04 · Gennaro Sardella · IV abciximab“the study was stopped because the sample size was very difficult to achieve.”
- terminated · 2012-03-22 · Bart Neyns · Cilengitide EMD 121974“Results of the phase III RTOG0525 trial made the manufacturer of cilengitide decide to end their support to the trial”
- terminated · 2011-05-17 · Centocor, Inc. · Abciximab“Based on the data and observed benefit-risk profile, the trial's independent oversight committee recommended that enrollment not resume.”
- terminated · 2009-01-09 · Archemix Corp. · matched by the registry's drug synonymsNo reason given
- terminated · 2007-12-06 · Attenuon · ATN-161No reason given
- terminated · 2007-05-03 · University of Zurich · Abciximab“Higher hemorrhage rates of Abciximab in ABESST II trial”
Paediatric incentives and obligations for ITGB3's drugs
For tirofiban, abciximab, zalunfiban, cilengitide, ATN-161, intetumumab, etaracizumab, tadocizumab, abituzumab: what EMA and FDA publish about paediatric plans, orphan status and pediatric approvals, and how many registered studies take children. Each line is a yes, no or not published fact from the record linked under it; none of it is a forecast.
- FDA pediatric target list: no · ITGB3 is not on the listRule: Target is on FDA's Pediatric Molecular Target List (relevant targets). Source: FDA Pediatric Molecular Target List (Listed as February 2026 on the FDA Pediatric Oncology page; the file served is 9.7.22_the_relevant_molecular_target_list.xlsx, whose Summary of Changes sheet is headed 'SEPTEMBER 2022 UPDATE' (footnote date 2022-09-01)), 2026-11-11
- EU paediatric investigation plan: yes · EMEA-000550-PIP02-10-M01 (cilengitide, Treatment of high-grade glioma): PM: decision on the application for modification of an agreed PIP, 1 Mar 2013Rule: An EMA PIP decision (agreement, modification or waiver) lists the drug as its active substance, exact name. Source: EMA EMEA-000550-PIP02-10-M01, 2026-11-11
- EU orphan designation: yes · EU/3/03/184 withdrawn 15 Jan 2004: Treatment of gliomaRule: An EU orphan designation lists the drug as its active substance (exact name) or belongs to a medicine that does; withdrawn and expired designations are listed with their status. Source: EMA EU/3/03/184, 2026-11-11
- Authorised in the EU: no · EMA lists no centrally authorised medicine of tirofiban, abciximab, zalunfiban, cilengitide, atn-161, intetumumab, etaracizumab, tadocizumab, abituzumabRule: An EMA medicine record lists the drug as its active substance or INN, exact name; national-only authorisations are not in this file. Source: EMA data download (dated snapshot), 2026-11-11
- FDA orphan designation: not published · FDA's orphan designation database turns away automated requests, so this app does not read it; search it by hand at the linkRule: Would be: an FDA orphan designation names the drug. Source: FDA orphan designations search
- FDA pediatric oncology approval: no · FDA's table lists no pediatric approval of tirofiban, abciximab, zalunfiban, cilengitide, atn-161, intetumumab, etaracizumab, tadocizumab, abituzumabRule: FDA's Pediatric Oncology Drug Approvals table names the drug. Source: FDA Pediatric Oncology Drug Approvals (content current as of 2026-03-03), 2026-11-11
- Registered studies open to children: yes · 11 interventional studies of tirofiban, abciximab, zalunfiban, cilengitide, atn-161, intetumumab, etaracizumab, tadocizumab, abituzumab include patients under 18; 0 are recruiting, not yet recruiting or activeRule: The registry's age group includes Child (birth to 17 years), which also counts studies that set no minimum age. Source: ClinicalTrials.gov search, 2026-11-11
Rare pediatric disease voucher. FDA, content current as of 29 Apr 2026: “As of February 3, 2026, enactment of the Consolidated Appropriations Act, 2026, the rare pediatric disease PRV program will sunset after September 30, 2029. FDA may not award any PRVs under this program after September 30, 2029.” Voucher sale prices are not shown here; they appear only as company-reported news. FDA: Rare Pediatric Disease Designation and Priority Review Voucher Programs
All 11 drugs and clinical candidates as a table
Each drug, stage and indication links to its Open Targets record, where the trials and approvals behind it are listed. Salt forms (for example a mesylate) are listed as Open Targets records them, as separate entries.