aplaviroc
Small moleculeexperimental
Aplaviroc is a CCR5 entry inhibitor that belongs to a class of 2,5-diketopiperazines developed for the treatment of HIV infection. It was developed by GlaxoSmithKline. — Wikipedia
Clinical trial activity
7 trials · 3 clinical orgs · 0 marketing orgs
Phase 1
0
Phase 2
7
Phase 3
4
Phase 4
0
Earliest trial started Jan 1, 2004 (NCT00076284)
Timeline
Indications
Studied for
Mechanism of action
- C-C chemokine receptor type 5ANTAGONIST
CCR5 antagonist
Discontinueddue to liver toxicity concerns.
Chemistry & pharmacology
Loading structure…
SMILES
CCCCN1C(=O)[C@@H]([C@H](O)C2CCCCC2)NC(=O)C12CCN(Cc1ccc(Oc3ccc(C(=O)O)cc3)cc1)CC2- Mol. weight
- 577.72 g/mol
- Lipinski Ro5
- 1 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL1255794 ↗
- WikipediaAplaviroc ↗
- ChEMBLCHEMBL1668019 ↗
Also known as
- 4-((4-(((3r)-1-butyl-3-((r)-cyclohexyl(hydroxy)methyl)-2,5-dioxo-1,4,9-triazaspiro(5.5)undec-9-yl)methyl)phenyl)oxy)benzoic acid hydrochloride
- aplaviroc
- aplaviroc
- aplaviroc
- aplaviroc hcl
- aplaviroc hcl
- aplaviroc hydrochloride
- aplaviroc hydrochloride
- benzoic acid, 4-(4-(((3r)-1-butyl-3-((r)-cyclohexylhydroxymethyl)-2,5-dioxo-1,4,9- triazaspiro(55)undec-9-yl)methyl)phenoxy)-
- gw873140
- gw873140
- gw873140
- gw873140a
- gw873140a
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00197145 | Phase 3 | Jul 1, 2005 | GlaxoSmithKline |
| NCT00297076 | Phase 3 | Jul 1, 2005 | GlaxoSmithKline |
| NCT00197197 | Phase 3 | Jul 1, 2005 | GlaxoSmithKline |
| NCT00123890 | Phase 3 | Jun 1, 2005 | GlaxoSmithKline |
| NCT00104429 | Phase 2 | Jan 1, 2005 | GlaxoSmithKline, ViiV Healthcare |
| NCT00102778 | Phase 2 | Dec 1, 2004 | GlaxoSmithKline, ViiV Healthcare |
| NCT00076284 | Phase 2 | Jan 1, 2004 | National Institute of Allergy and Infectious Diseases (NIAID) |
Showing 7 of 7 trials
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Organizations
Research & Development (3)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| GlaxoSmithKline | For profit | 6 | 4 | 2 | 2004 |
| ViiV Healthcare | For profit | 2 | 2 | 1 | 2004 |
| National Institute of Allergy and Infectious Diseases (NIAID) | Government | 1 | 1 | 1 | 2004 |
3 organizations
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