F2 coagulation factor II, thrombin
ENSG00000180210 · protein coding · Open Targets profile
Thrombin, which cleaves bonds after Arg and Lys, converts fibrinogen to fibrin and activates factors V, VII, VIII, XIII, and, in complex with thrombomodulin, protein C. Functions in blood homeostasis, inflammation and wound healing. Activates coagulation factor XI (F11); activation is promoted by the contact with negatively charged surfaces (PubMed:2019570, PubMed:21976677). Triggers the production of pro- inflammatory cytokines, such as MCP-1/CCL2 and IL8/CXCL8, in endothelial cells (PubMed:30568593, PubMed:9780208). {ECO:0000269|PubMed:2019570, ECO:0000269|PubMed:21976677, ECO:0000269|PubMed:2856554, ECO:0000269|PubMed:30568593, ECO:0000269|PubMed:9780208}.
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 Withdrawn means the drug was pulled from the market or from development.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, High-Quality Pocket, Druggable Family
- Antibody
- Advanced Clinical, GO CC high conf, UniProt loc med conf, UniProt SigP or TMHMM
- PROTAC
- Half-life Data, Small Molecule Binder
- Other modalities
- Approved Drug
gnomAD loss of function constraint: o/e 0.4153200089931488 (upper bound 0.5529299974441528). 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 233 registry trials, updated in the last three years, of the most advanced drugs against F2 (defibrotide, prothrombin, dabigatran etexilate, argatroban, dabigatran, prothrombin complex concentrate, atecegatran metoxil), ranked by Phase 2+ trials. Live from ClinicalTrials.gov.
- Lei ZhangInstitute of Hematology & Blood Diseases Hospital Chinese Academy of Medical Sciences & Peking Union Medical College · 2 of 6 trials Phase 2+
- Amy D ShapiroIndiana Hemophilia &Thrombosis Center, Inc. · 2 of 2 trials Phase 2+
- David ChiuNYU Langone Health · 2 of 2 trials Phase 2+
- Gunnar H GislasonDanish Heart Foundation · 2 of 2 trials Phase 2+
- Mitchell CairoNew York Medical College · 2 of 2 trials Phase 2+
- mohamed G. Zeinhomneurology department kafr el-sheikh university · 2 of 2 trials Phase 2+
- Steven PipeUniversity of Michigan · 2 of 2 trials Phase 2+
- Annetine C GelijnsIcahn School of Medicine at Mount Sinai · 1 of 1 trials Phase 2+
- Arvindh N KanagasundramVanderbilt University Medical Center · 1 of 1 trials Phase 2+
- Asishana A OshoMassachusetts General Hospital · 1 of 1 trials Phase 2+
- Athan KuliopulosTufts Medical Center · 1 of 1 trials Phase 2+
- Azmi RahmanSingapore General Hospital · 1 of 1 trials Phase 2+
- Banne NemethLeiden University Medical Center · 1 of 1 trials Phase 2+
- Caifeng YangShanghai Xinzhi BioMed Co., Ltd. · 1 of 1 trials Phase 2+
- Caroline OzmentDuke University · 1 of 1 trials Phase 2+
Registry trials of defibrotide, prothrombin, dabigatran etexilate, argatroban, dabigatran, prothrombin complex concentrate, atecegatran metoxil 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; 183 of 221 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. 12 trials list no sites and are left out. Source: ClinicalTrials.gov, fetched live.
108 trials of drugs against F2 were stopped early; 18 give no reason
Terminated, withdrawn and suspended interventional trials of defibrotide, prothrombin, dabigatran etexilate, argatroban, dabigatran, prothrombin complex concentrate, atecegatran metoxil, ichorcumab, 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 108.
- terminated · 2026-11-10 · University of Maryland, Baltimore · matched by the registry's drug synonyms“Standard practice change prohibited enrollment”
- withdrawn · 2026-11-06 · Emory University · matched by the registry's drug synonyms“The study was withdrawn because the pharmaceutical sponsor withdrew support for the study. No participants were enrolled before termination.”
- terminated · 2026-10-21 · University Health Network, Toronto · matched by the registry's drug synonyms“Upon IDSMC's review of interim data, they recommended the trial be stopped based on futility.”
- terminated · 2026-10-07 · Instituto Grifols, S.A. · matched by the registry's drug synonyms“Due to recruitment challenges during the trial, this study was terminated early by the Sponsor.”
- terminated · 2026-10-05 · Pfizer · matched by the registry's drug synonyms“The study was terminated early due to Sponsor and participants may transition into a long-term follow-up study. The decision to terminate the trial was not based on any safety and/or efficacy concerns.”
- terminated · 2026-07-31 · Spur Therapeutics · matched by the registry's drug synonyms“Freeline has decided to pause development of FLT180a for business priorities”
- terminated · 2026-07-24 · AstraZeneca · matched by the registry's drug synonyms“The study terminated because the clinical development programme for Ceralasertib has been discontinued.”
- terminated · 2026-06-25 · Octapharma · matched by the registry's drug synonyms“Following Interim Analysis IDMEAC concluded:1-No safety concerns 2-Suspend enrolment: Futility based on treatment effect size at interim analysis. Enrollment was suspended on 22DEC25. Study was terminated FEB2026. Final analysis is planned in Q2 2026”
- terminated · 2026-06-24 · SHI Jia · Prothrombin Complex Concentrate, Human“At a meeting on February 17, 2025, the Data and Safety Monitoring Board recommended early termination because the predefined efficacy boundary was crossed.”
- withdrawn · 2026-05-12 · Bayer · Dabigatran etexilate“The study is no longer required.”
- terminated · 2025-12-10 · CSL Behring · matched by the registry's drug synonyms“Study was terminated early because mortality was lower than expected and a significant increase in sample size would have been required to meet statistical goals of the study. No safety reasons were involved in the decision to terminate the study.”
- withdrawn · 2025-11-04 · Brian O'Neill MD · Market approved oral anticoagulation (OAC), such as warfarin (Coumadin), dabigatran (Pradaxa), rivaroxaban (Xarelto), apixiban (Eliquis), edoxaban (Savaysa), or betrixaban (Bevyxxa)“Lack of Funding”
- withdrawn · 2025-04-22 · ViiV Healthcare · matched by the registry's drug synonyms“Sponsor decision”
- withdrawn · 2025-04-17 · University of Rhode Island · Dabigatran“Investigator left institution”
- terminated · 2024-12-27 · National Hospital Organization Osaka National Hospital · matched by the registry's drug synonyms“The trial was terminated at the planned interim analysis for futility on July 18, 2023.”
- terminated · 2024-11-15 · Pfizer · Dabigatran etexilate (DE)“The decision to terminate clinical development of lotiglipron is based on pharmacokinetic data from Phase 1 drug-drug-interaction studies and laboratory measurements of elevated transaminases in these Phase 1 studies as well as a Phase 2 study.”
- terminated · 2024-11-15 · University of Texas Southwestern Medical Center · matched by the registry's drug synonyms“Study enrollment ceased because this was enrolling as a pilot study until a larger study (FUVID) was submitted, approved and received funding.”
- withdrawn · 2024-08-07 · University of California, San Francisco · Defibrotide“Industry sponsor decision”
- terminated · 2024-07-19 · Sangamo Therapeutics · matched by the registry's drug synonymsNo reason given
- terminated · 2024-06-26 · NYU Langone Health · matched by the registry's drug synonyms“Both lack of enrollment as well as study staff turnover”
- terminated · 2024-06-04 · Sunnybrook Health Sciences Centre · matched by the registry's drug synonyms“Study terminated due to logistical challenges in conducting the trial.”
- terminated · 2024-04-18 · Hospices Civils de Lyon · matched by the registry's drug synonyms“More Hardware”
- terminated · 2024-04-11 · Indiana Hemophilia &Thrombosis Center, Inc. · matched by the registry's drug synonyms“Global COVID-19 pandemic prevented further study visits or enrollment.”
- terminated · 2023-10-18 · HonorHealth Research Institute · matched by the registry's drug synonyms“Study was closed due to low subject enrollment at site.”
- terminated · 2023-09-29 · ImPACT Applications, Inc. · matched by the registry's drug synonyms“Loss of funding.”
Paediatric incentives and obligations for F2's drugs
For defibrotide, prothrombin, dabigatran etexilate, argatroban, dabigatran, prothrombin complex concentrate, atecegatran metoxil, ichorcumab: 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 · F2 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-000081-PIP01-07-M11 (dabigatran etexilate mesilate, Prevention of thromboembolic events;Treatment of thromboembolic events): PM: decision on the application for modification of an agreed PIP, 7 Dec 2018; compliance positive 23 Aug 2019Rule: An EMA PIP decision (agreement, modification or waiver) lists the drug as its active substance, exact name. Source: EMA EMEA-000081-PIP01-07-M11, 2026-11-11
- EU orphan designation: yes · EU/3/04/211 withdrawn 29 Jul 2004: Prevention of hepatic veno-occlusive disease; EU/3/13/1201 withdrawn 13 Nov 2013: Prevention of graft-versus-host disease; EU/3/04/212 positive 29 Jul 2004: Treatment of hepatic veno-occlusive diseaseRule: 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 data download (dated snapshot), 2026-11-11
- Authorised in the EU: yes · Pradaxa: authorised since 17 Mar 2008; Dabigatran Etexilate Accord: authorised since 26 May 2023; Dabigatran etexilate Teva (previously Dabigatran etexilate Leon Farma): authorised since 19 Feb 2024; Dabigatran etexilate Teva: application withdrawn; +1 moreRule: 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 defibrotide, prothrombin, dabigatran etexilate, argatroban, dabigatran, prothrombin complex concentrate, atecegatran metoxil, ichorcumabRule: FDA's Pediatric Oncology Drug Approvals table names the drug. Source: FDA Pediatric Oncology Drug Approvals (content current as of 2026-03-03), 2026-11-12
- Registered studies open to children: yes · 150 interventional studies of defibrotide, prothrombin, dabigatran etexilate, argatroban, dabigatran, prothrombin complex concentrate, atecegatran metoxil, ichorcumab include patients under 18; 19 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, 2026-11-12
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 14 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.