Home Microbiology Reverse Transcriptase inhibitor Dapivirine (TMC120)

Dapivirine (TMC120)

Catalog No.S2914

For research use only.

Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. Phase 3.

Dapivirine (TMC120) Chemical Structure

CAS No. 244767-67-7

Selleck's Dapivirine (TMC120) has been cited by 9 Publications

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Biological Activity

Description Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. Phase 3.
Targets
HIV reverse transcriptase [1]
24 nM
In vitro

Dapivirine prevents HIV-induced syncytium formation in the nanomolar range and shows a low cytostatic activity. Dapivirine apparently blocks HIV-1 infection in the primary cultures at a 10 nM concentration, but secondary cultures reveals that a 100 nM concentration is needed to completely prevent proviral integration. [1] Dapivirine is well tolerated by epithelial cells, T cells, macrophages, and cervical tissue explants with CC50 (50% cytotoxic concentration) of 10 μM to 20 μM. Dapivirine potently inhibits infection by both X4- and R5-utilizing HIV-1 strains with IC50 of 1.46 nM in cell-based assays. Dapivirine potently inhibits HIV-1BaL infection of human ectocervical explant tissue in a dose-dependent manner, as evaluated by the reduction in both p24 release and provirus content in cultured explants. Dapivirine inhibits the transmission of virus to permissive T cells in a dose-dependent manner, with an IC50 of 0.1 nM. Dapivirine results in significant inhibition of HIV infection when explants are challenged with virus immediately with IC90 of 100 nM. Dapivirine is also able to inhibit viral dissemination by migratory cells. [2]
In vivo Dapivirine-containing gel at vaginal level inhibits cell-associated HIV infection in mice. [3] More placebo (7 of 12) than Dapivirine (3 of 24) gel users has positive vaginal swab results, with white blood cells being the most common finding. Dapivirine (0.05%) results in Cmax of 715 pg/mL, AUC of 15 ng×h/mL and T1/2 of 89.87 hours in plasma after 14 days post-dose. Mean Dapivirine (0.05%) concentrations in vaginal fluids collected at the introitus, mid vagina, and cervix are in the range of 62-265 μg/g on day 1. [4]

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 329.4
Formula

C20H19N5
CAS No. 244767-67-7
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=C(C(=C1)C)NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03593655 Completed Device: Dapivirine vaginal ring|Drug: FTC/TDF HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) January 14 2019 Phase 2
NCT03393468 Completed Drug: Dapivirine gel HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) May 10 2018 Phase 1
NCT03239483 Completed Drug: Dapivirine gel|Drug: Placebo gel HIV Infections National Institute of Allergy and Infectious Diseases (NIAID) October 26 2017 Phase 1
NCT02858037 Completed Combination Product: Dapivirine Vaginal Ring Human Immunodeficiency Virus International Partnership for Microbicides Inc. August 2016 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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