fostemsavir
Trade name: Rukobia
Approved
Jul 2, 2020
Fostemsavir, sold under the brand name Rukobia, is an antiretroviral medication for adults living with HIV/AIDS who have tried multiple HIV medications and whose HIV infection cannot be successfully treated with other therapies because of resistance, intolerance or safety considerations. — Wikipedia
Clinical trial activity
30 trials · 17 clinical orgs · 1 marketing orgs
Earliest trial started Nov 1, 2009 (NCT01009814)
Timeline
2000s
- Jan 1, 2009
Earliest Phase 2 Sponsor(trial)
2010s
- Jan 1, 2013
Earliest Phase 1 Sponsor(trial)
- Jan 1, 2015
ViiV Healthcare — Earliest Phase 3 Sponsor(trial)
2020s
- Jul 2, 2020
ViiV Healthcare — Earliest FDA Approval
- Jul 2, 2020
ViiV Healthcare — Marketing Organization
- Jul 2, 2020
ViiV Healthcare — NDA Secondary Org
- Jul 2, 2020
ViiV Healthcare — NDA Organization
Indications
Studied for
- Bone Marrow Diseases · Phase 1
- Heart Disease Risk Factors · Phase 2
- Hematologic Diseases · Phase 1
- Hematologic Neoplasms · Phase 3
- HIV · Phase 2
- HIV Infections · Phase 4
- Leukemia · Phase 1
- Leukemia, Myeloid, Acute · Phase 1
- Lymphoma · Phase 3
- Multiple Myeloma · Phase 1
- Myelodysplastic Syndromes · Phase 1
- Myeloproliferative Disorders · Phase 1
- Neoplasms · Phase 3
- Neoplasms by Histologic Type · Phase 1
- Peripheral Nervous System Neoplasms · Phase 2
- Polycythemia Vera · Phase 3
- Precancerous Conditions · Phase 1
- Preleukemia · Phase 1
- Primary Myelofibrosis · Phase 3
- Thrombocytosis · Phase 1
Mechanism of action
- Envelope glycoproteinANTAGONIST
Envelope glycoprotein antagonist
- Envelope glycoprotein D (gD) ↗
- Envelope glycoprotein B (gB) ↗
- Envelope glycoprotein C (gC) ↗
- Envelope glycoprotein E (gE) ↗
- Envelope glycoprotein G (gG) ↗
- Envelope glycoprotein H (gH) ↗
- Envelope glycoprotein I (gI) ↗
- Envelope glycoprotein J (gJ) ↗
- Envelope glycoprotein K (gK) ↗
- Envelope glycoprotein L (gL) ↗
- Envelope glycoprotein M (gM) ↗
- Envelope glycoprotein N (gN) ↗
- Envelope polyprotein GP160INHIBITOR
Envelope polyprotein GP160 inhibitor
Binds the gp120 subunit of the viral gp160 envelope glycoprotein and inhibits attachment to host CD4 receptors. Also inhibits other gp120-dependent post-attachment steps.
Activity varied depending on tropism, less active against subtype AE.
gp120 subunit
Bromodomain and extra-terminal motif (BET) inhibitor
Approval history
- approvedPriority reviewFast trackBreakthroughJul 2, 2020
Chemistry & pharmacology
SMILES
COc1cnc(-n2cnc(C)n2)c2c1c(C(=O)C(=O)N1CCN(C(=O)c3ccccc3)CC1)cn2COP(=O)(O)O- Mol. weight
- 583.5 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Achiral Molecule
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaFostemsavir ↗
- ChEMBLCHEMBL4303404 ↗
- ChEMBLCHEMBL3301598 ↗
- ChEMBLCHEMBL3301594 ↗
Also known as
- bms-663068
- bms-663068
- bms-663068
- cpi-0610
- cpi-0610
- fostemsavir
- fostemsavir
- fostemsavir
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT07030920 | Phase 2 | Sep 30, 2025 | BC Women's Hospital & Health Centre, Clinique du Quartier Latin, McGill University, University of Montreal |
| NCT07053384 | Phase 1 | Jul 10, 2025 | ViiV Healthcare |
| NCT06401356 | Phase 3 | Aug 13, 2024 | Constellation Pharmaceuticals |
| NCT05220358 | Phase 4 | May 1, 2022 | Orlando Immunology Center, ViiV Healthcare |
| NCT05391022 | Phase 1 | Jul 26, 2021 | Constellation Pharmaceuticals |
| NCT04648280 | Phase 1/Phase 2 (Phase 2) | Jun 30, 2021 | Cromsource, PENTA Foundation, PHPT Foundation, Universidad Complutense de Madrid, ViiV Healthcare |
| NCT04757974 | Phase 1 | Mar 5, 2021 | ViiV Healthcare |
| NCT04603495 | Phase 3 | Nov 19, 2020 | Constellation Pharmaceuticals |
| NCT02986919 | Phase 2 | Apr 1, 2017 | The University of Texas, Dallas |
| NCT02859259 | Phase 1 | Aug 12, 2016 | ViiV Healthcare |
| NCT02805556 | Phase 1 | Mar 15, 2016 | GlaxoSmithKline, ViiV Healthcare |
| NCT02674581 | Phase 1 | Mar 10, 2016 | Covance, GlaxoSmithKline, ViiV Healthcare |
| NCT02666001 | Phase 1 | Jan 1, 2016 | GlaxoSmithKline, ViiV Healthcare |
| NCT02666053 | Phase 1 | Jan 1, 2016 | Bristol-Myers Squibb |
| NCT02508064 | Phase 1 | Aug 1, 2015 | Bristol-Myers Squibb |
| NCT02480894 | Phase 1 | Jul 1, 2015 | Bristol-Myers Squibb |
| NCT02480881 | Phase 1 | Jul 1, 2015 | Bristol-Myers Squibb |
| NCT02467335 | Phase 1 | Jun 1, 2015 | Bristol-Myers Squibb |
| NCT02362503 | Phase 3 | Mar 1, 2015 | ViiV Healthcare |
| NCT02277600 | Phase 1 | Nov 5, 2014 | GlaxoSmithKline, ViiV Healthcare |
Organizations
Research & Development (17)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| ViiV Healthcare | For profit | 13 | 11 | 5 | 2014 |
| Bristol-Myers Squibb | For profit | 9 | 9 | 2 | 2009 |
| Constellation Pharmaceuticals | For profit | 6 | 6 | 2 | 2013 |
| GlaxoSmithKline | For profit | 6 | 0 | 1 | 2014 |
| The Leukemia and Lymphoma Society | Academic/Hospital | 3 | 0 | 1 | 2013 |
| BC Women's Hospital & Health Centre | Academic/Hospital | 1 | 0 | 1 | 2025 |
| Clinique du Quartier Latin | Academic/Hospital | 1 | 0 | 1 | 2025 |
| Covance | For profit | 1 | 0 | 1 | 2016 |
| Cromsource | For profit | 1 | 0 | 1 | 2021 |
| McGill University | Academic/Hospital | 1 | 0 | 1 | 2025 |
| Orlando Immunology Center | Academic/Hospital | 1 | 1 | 1 | 2022 |
| PENTA Foundation | Academic/Hospital | 1 | 1 | 1 | 2021 |
| PHPT Foundation | Academic/Hospital | 1 | 0 | 1 | 2021 |
| PPD | For profit | 1 | 0 | 1 | 2014 |
| The University of Texas, Dallas | Academic/Hospital | 1 | 1 | 1 | 2017 |
| Universidad Complutense de Madrid | Academic/Hospital | 1 | 0 | 1 | 2021 |
| University of Montreal | Academic/Hospital | 1 | 1 | 1 | 2025 |
Marketing (3)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| ViiV Healthcare | For profit | MKTG | Jul 2, 2020 |
| ViiV Healthcare | For profit | NDA2 | Jul 2, 2020 |
| ViiV Healthcare | For profit | NDA | Jul 2, 2020 |