peptide t
Peptide T is an HIV entry inhibitor discovered in 1986 by Candace Pert and Michael Ruff, a US neuroscientist and immunologist. Peptide T, and its modified analog Dala1-peptide T-amide (DAPTA), a drug in clinical trials, is a short peptide derived from the HIV envelope protein gp120 which blocks binding and infection of viral strains which use the CCR5 receptor to infect cells. DAPTA was initially administered as a nasal spray, but this formulation was found to be unstable. A more stable oral form, called RAP-103, is a shorter pentapeptide derived from DAPTA. RAP-103 is a CCR2/CCR5 antagonist that protects synapses by blocking the synaptotoxic actions of oligomeric forms of amyloid beta and alpha-synuclein., as well as HIV gp120, via a PrPc dependent pathway. Synapse loss underlies the cognitive losses attributed to these toxic proteins and the ensuing clinical conditions of AD, LBD, and HAND, which these peptide chemokine receptor antagonists may safely treat. In preclinical studies, RAP-103 has also been shown to prevent and reverse neuropathic pain and to reduce opioid addiction liability. — Wikipedia
Clinical trial activity
4 trials · 2 clinical orgs · 0 marketing orgs
Earliest trial started Jan 1, 1988 (NCT00000393)
Timeline
Indications
Mechanism of action
- Envelope glycoprotein gp160INHIBITOR
Q993A8 inhibitor
Chemistry & pharmacology
SMILES
C[C@H](N)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O- Mol. weight
- 857.87 g/mol
- Lipinski Ro5
- 3 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Multi-specific
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaPeptide T ↗
- ChEMBLCHEMBL180971 ↗
Also known as
- peptide t
- peptide t
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00002083 | N/A | Nov 2, 1999 | Advanced Peptides |
| NCT00000392 | Phase 2 | Jan 1, 1990 | National Institute of Mental Health (NIMH) |
| NCT00000391 | Phase 1 | Jan 1, 1988 | National Institute of Mental Health (NIMH) |
| NCT00000393 | Phase 1 | Jan 1, 1988 | National Institute of Mental Health (NIMH) |
Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| National Institute of Mental Health (NIMH) | Government | 3 | 3 | 2 | 1988 |
| Advanced Peptides | For profit | 1 | 1 | 1 | 1999 |