| Name | IQP-0528 |
| Description | IQP-0528 is a potent non-nucleoside reverse transcriptase inhibitor (NNRTI) that has potential for the treatment of HIV infection by blocking viral entry and shows antiviral activity as a microbicidal gel. . IQP-0528 showed inhibition of both HIV-1 and HIV-2, with an EC50 of 0.2 nM for HIV-1 and 100 nM for HIV-2. |
| In vitro | The in vitro safety evaluations showed no significant loss in cell viability or significant inflammatory response after treatment with a 3.0% HEC gel containing 0.25% IQP-0528. In an in vitro HIV-1 entry inhibition assay, the lead formulation showed an 50% effective concentration of 0.14 μg/ml for gel in culture media, which corresponds to ∼0.001 μM IQP-0528.[5] |
| In vivo | we report the first-in-human evaluation of such a gel containing 1% IQP-0528, an investigational antiretroviral. Seven HIV-1-negative participants received one 10 mL rectal dose of radiolabeled 1% IQP-0528 gel. Median IQP-0528 concentrations in rectal tissue exceeded the in vitro EC95 against HIV-1 (0.07 ng/mg) by 3-5 h of dosing and remained above this concentration for at least 24 h, despite a 3-log reduction in concentration over this duration of time. Rectal tissue PD assessed by ex vivo HIV challenge-demonstrated significant p24 antigen reduction 3-5 h postdose compared with baseline , but not 24-26 h postdose. The IQP-0528 gel possesses desirable features for a topical microbicide including local safety with no systemic absorption, delivery of locally high IQP-0528 concentrations, and significant reductions in ex vivo HIV infectivity.[6] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 4 mg/mL (11.75 mM), Sonication is recommended.
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| Keywords | SJ 3991 | ReverseTranscriptase | Reverse Transcriptase | Nucleoside reverse transcriptase | IQP-0528 | IQP 0528 | HIVProtease | HIV Protease | Antiviral |
| Inhibitors Related | Stavudine | 5-Fluorouracil | Emtricitabine | Dolutegravir intermediate-1 | Dimethyl fumarate | Hexane-2,5-dione | Lamivudine | Sodium formate | Valproic Acid | (-)-Epigallocatechin Gallate | Decanedioic acid | Dextran sulfate sodium salt (MW 5000) |
| Related Compound Libraries | Bioactive Compound Library | ReFRAME Related Library | Multi-Target Compound Library | Anti-Viral Compound Library | Inhibitor Library | Immunology/Inflammation Compound Library | Bioactive Compounds Library Max | Anti-Infection Compound Library |
United States
