Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Design and evaluation of sifuvirtide, a novel HIV-1 fusion inhibitor. | 2008 Apr 25 |
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| Sifuvirtide, a potent HIV fusion inhibitor peptide. | 2009 May 8 |
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| Resistance profiles of novel electrostatically constrained HIV-1 fusion inhibitors. | 2010 Dec 10 |
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| Short-peptide fusion inhibitors with high potency against wild-type and enfuvirtide-resistant HIV-1. | 2013 Mar |
| Substance Class |
Protein
Created
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admin
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Edited
Sat Dec 16 14:11:03 GMT 2023
by
admin
on
Sat Dec 16 14:11:03 GMT 2023
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| Protein Type | PEPTIDE |
| Protein Sub Type | |
| Sequence Type | COMPLETE |
| Record UNII |
5LJI43ULT6
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| Record Status |
Validated (UNII)
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| Record Version |
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5LJI43ULT6
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857094-21-4
Created by
admin on Sat Dec 16 14:11:03 GMT 2023 , Edited by admin on Sat Dec 16 14:11:03 GMT 2023
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Unlike T20, sifuvirtide could efficiently
block six-helix bundle formation in a dominant negative fashion. These results suggest that sifuvirtide has a different mechanism of action from that of T20. Phase Ia clinical studies of sifuvirtide(FS0101) in 60 healthy individuals demonstrated good safety, tolerability, and pharmacokinetic profiles. A single dose regimen(5, 10, 20, 30, and 40mg) by subcutaneous injection once daily at abdominal sites was well tolerated without serious adverse events. Pharmacokinetic studies of single and multiple administration of sifuvirtide showed that its decay half-lives were 20.08.6 h and 26.07.9 h, respectively. In summary, sifuvirtide has potential
to become an ideal fusion inhibitor for treatment of HIV/AIDS patients, including those with HIV-1 strains resistant to T20.
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ACTIVE MOIETY |
The pharmacokinetics assessment in two clinical studies of sifuvirtide (a novel HIV fusion inhibitor) was first reported in Chinese HIV patients. Nineteen treatment-naive HIV patients were treated with s.c.(subcutaneous injection) sifuvirtide (10 or 20 mg q.d.(quaque die)) for 28 days in study 1, and eight treatment-experienced HIV patients were treated with s.c. sifuvirtide (20 mg q.d.) in combination with HAART drugs (lamivudine, didanosine, and Kaletra) for 168 days in study 2. In study 1, T1/2 was 17.8 +/- 3.7 h for 10 mg group and 39.0 +/- 3.5 h for 20 mg group the mean Cmax of last dose was 498 +/- 54 ng/mL for 10 mg group and 897 +/- 136 ng/mL for 20 mg group. In study 2, T1/2 was 6.71 +/- 2.17 h in treatment-experienced patients. Cmax was 765 +/- 288 ng/mL after last 168th dosage. Sifuvirtide showed improved clinical pharmacokinetics characteristics compared with Enfuvirtide, and showed very different pharmacokinetic characteristics between treatment-naive and treatment-experienced patients.
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ACTIVE MOIETY |
Class: Antiviral, Peptide; Mechanism of Action: HIV fusion inhibitor; Highest Development Phase: Phase II for HIV infections; Most Recent Events: 25 Jun 2015 Sifuvirtide is still in preclinical trials for HIV infections (Prevention) in China (Topical), 25 Jun 2015 Sifuvirtide is still in phase II trials for HIV infections in China (SC), 01 Aug 2010 Safety and efficacy data from four completed phase I-II trials released by FusoGen Pharmaceuticals
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ACTIVE MOIETY |
Indication: HIV infection; Focus: Adverse reactions; Sponsor: FusoGen Pharmaceuticals; Most Recent Events: 01 Aug 2010 An update of FusoGen's sifuvirtide development programme was presented at a symposium in Beijing, according to a FusoGen Pharmaceuticals media release.
13 Jul 2009 New trial record.
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| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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| Molecular Formula | CHEMICAL |
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