vinflunine
Small moleculeexperimental
Vinflunine is a novel fluorinated vinca alkaloid derivative undergoing research for the treatment of bladder cancer. It was originally discovered by the team of the Professor Jean-Claude Jacquesy, developed by Laboratoires Pierre Fabre and was licensed to Bristol-Myers Squibb for development in certain countries, including the United States. — Wikipedia
Clinical trial activity
32 trials · 26 clinical orgs · 0 marketing orgs
Phase 1
7
Phase 2
24
Phase 3
14
Phase 4
0
Earliest trial started Jan 1, 2005 (NCT00101608)
Timeline
Indications
Studied for
- Breast Neoplasms · Phase 3
- Carcinoma, Non-Small-Cell Lung · Phase 2
- Carcinoma, Small Cell · Phase 2
- Carcinoma, Transitional Cell · Phase 3
- Kidney Neoplasms · Phase 2
- Lung Neoplasms · Phase 2
- Neoplasm Metastasis · Phase 3
- Penile Neoplasms · Phase 2
- Prostatic Neoplasms · Phase 2
- Squamous Cell Carcinoma of Head and Neck · Phase 3
- Stomach Neoplasms · Phase 2/Phase 3
- Ureteral Neoplasms · Phase 3
- Urethral Neoplasms · Phase 2
- Urinary Bladder Neoplasms · Phase 3
Mechanism of action
- TubulinINHIBITOR
Tubulin inhibitor
VFL bound to tubulin induces structural changes favoring an inhibition of GTP hydrolysis and inhibition of microtubule assembly
Interacts with the so-called vinca-alkaloid-binding-domain of tubulin
- Tubulin beta-4B chain (TUBB4B) ↗
- Tubulin beta-1 chain (TUBB1) ↗
- Tubulin alpha-3C chain (TUBA3C) ↗
- Tubulin alpha-4A chain (TUBA4A) ↗
- Tubulin beta-3 chain (TUBB3) ↗
- Tubulin alpha-1A chain (TUBA1A) ↗
- Tubulin beta-4A chain (TUBB4A) ↗
- Tubulin beta-8 chain (TUBB8) ↗
- Tubulin beta chain (TUBB) ↗
- Tubulin alpha-1B chain (TUBA1B) ↗
- Tubulin alpha-1C chain (TUBA1C) ↗
- Tubulin alpha-3E chain (TUBA3E) ↗
- Tubulin beta-2A chain (TUBB2A) ↗
- Tubulin beta-2B chain (TUBB2B) ↗
- Tubulin beta-6 chain (TUBB6) ↗
Chemistry & pharmacology
Loading structure…
SMILES
CC[C@]12C=CCN3CC[C@@]4(c5cc([C@@]6(C(=O)OC)C[C@@H]7C[C@@H](C(C)(F)F)CN(Cc8c6[nH]c6ccccc86)C7)c(OC)cc5N(C)[C@H]4[C@@](O)(C(=O)OC)[C@@H]1OC(C)=O)[C@@H]32- Mol. weight
- 816.94 g/mol
- Lipinski Ro5
- 3 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaVinflunine ↗
- ChEMBLCHEMBL2218881 ↗
- ChEMBLCHEMBL2110725 ↗
Also known as
- javlor
- javlor
- vinflunine
- vinflunine
- vinflunine
- vinflunine
- vinflunine
- vinflunine
- vinflunine
- vinflunine
- vinflunine ditartrate
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT04527991 | Phase 3 | Nov 16, 2020 | Immunomedics |
| NCT03474107 | Phase 3 | Jun 27, 2018 | Astellas, Seattle Genetics |
| NCT03390504 | Phase 3 | Mar 23, 2018 | Johnson and Johnson |
| NCT02845050 | Phase 1/Phase 2 (Phase 2) | Jul 1, 2016 | Association of Urogenital Oncology (AUO) |
| NCT02302807 | Phase 3 | Jan 13, 2015 | Roche |
| NCT02256436 | Phase 3 | Oct 22, 2014 | Merck |
| NCT02665039 | Phase 2 | Apr 1, 2014 | Karolinska Institute |
| NCT02347332 | Phase 3 | Apr 1, 2014 | Pierre Fabre |
| NCT02057913 | Phase 2 | Mar 1, 2014 | University of London |
| NCT01953003 | Phase 3 | Sep 1, 2013 | Chinese Academy of Medical Sciences, Pierre Fabre |
| NCT01830231 | Phase 2/Phase 3 (Phase 3) | Oct 1, 2012 | Associació per a la Recerca Oncologica, Spain |
| NCT01844947 | Phase 1 | Jun 1, 2012 | Bayer, Karolinska Institute, Nordic Urothelial Cancer Oncology Group, Pierre Fabre |
| NCT01529411 | Phase 2 | Feb 1, 2012 | Badalona Hospital Germans Trias i Pujol, Hospital Universitario Fundación Alcorcón, Spanish Oncology Genito-Urinary Group |
| NCT01265940 | Phase 1/Phase 2 (Phase 2) | Mar 1, 2011 | Lukas-Krankenhaus GmbH |
| NCT01599013 | Phase 2 | Feb 1, 2011 | Kaiser Franz Josef Hospital, Pierre Fabre, University of Paris |
| NCT01091168 | Phase 3 | Sep 1, 2009 | Pierre Fabre |
| NCT01095003 | Phase 3 | May 1, 2009 | Pierre Fabre |
| NCT00534807 | Phase 1 | Sep 1, 2007 | Bristol-Myers Squibb |
| NCT00519831 | Phase 2 | Aug 1, 2007 | Bristol-Myers Squibb, University of North Carolina at Chapel Hill |
| NCT00545766 | Phase 2 | May 1, 2007 | Bristol-Myers Squibb, SCRI Development Innovations |
Showing 20 of 32 trials
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Organizations
Research & Development (26)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Bristol-Myers Squibb | For profit | 12 | 6 | 3 | 2005 |
| Pierre Fabre | For profit | 9 | 7 | 3 | 2005 |
| SCRI Development Innovations | For profit | 3 | 3 | 1 | 2006 |
| Karolinska Institute | Academic/Hospital | 2 | 2 | 2 | 2012 |
| National Cancer Institute (NCI) | Government | 2 | 1 | 2 | 2006 |
| University of North Carolina at Chapel Hill | Academic/Hospital | 2 | 2 | 2 | 2006 |
| Associació per a la Recerca Oncologica, Spain | Academic/Hospital | 1 | 1 | 1 | 2012 |
| Association of Urogenital Oncology (AUO) | Academic/Hospital | 1 | 1 | 1 | 2016 |
| Astellas | For profit | 1 | 1 | 1 | 2018 |
| Badalona Hospital Germans Trias i Pujol | Academic/Hospital | 1 | 0 | 1 | 2012 |
| Bayer | For profit | 1 | 0 | 1 | 2012 |
| Chinese Academy of Medical Sciences | Academic/Hospital | 1 | 0 | 1 | 2013 |
| Hospital Universitario Fundación Alcorcón | Academic/Hospital | 1 | 0 | 1 | 2012 |
| Immunomedics | For profit | 1 | 1 | 1 | 2020 |
| Johnson and Johnson | For profit | 1 | 1 | 1 | 2018 |
| Kaiser Franz Josef Hospital | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Lukas-Krankenhaus GmbH | Academic/Hospital | 1 | 1 | 1 | 2011 |
| Mayo Clinic | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Merck | For profit | 1 | 1 | 1 | 2014 |
| Nordic Urothelial Cancer Oncology Group | Academic/Hospital | 1 | 0 | 1 | 2012 |
26 organizations
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