BI 224436 is a novel HIV-1 noncatalytic site integrase inhibitor with EC50 values of less than 15 nM against different HIV-1 laboratory strains.
(+)-Carbovir triphosphate is an enantiomer of Carbovir triphosphate (HY-131607). (+)-Carbovir triphosphate is an inhibitor and substrate of HIV reverse transcriptase[1].
GS-6207 is a HIV-1 capsid inhibitor. GS-6207 shows anti-HIV activity with an EC50 of 100 pM in MT-4 cells. GS-6207 displays a mean EC50 of 50 pM (20-160 pM) against 23 HIV-1 clinical isolates from different subtypes in peripheral blood mononuclear cells (PBMCs)[1].
AMD 3465 hexahydrobromide is a potent antagonist of CXCR4, inhibits binding of 12G5 mAb and CXCL12AF647 to CXCR4, with IC50s of 0.75 nM and 18 nM in SupT1 cells; AMD 3465 also potently inhibits the replication of X4 HIV strains (IC50: 1-10 nM), but has no effect on CCR5-using (R5) viruses.
Darunavir ethanolate (TMC114 ethanolate) is a potent HIV protease inhibitor used to treat and prevent HIV/AIDS. Darunavir has a Ki of 1 nM for wild type HIV-1 protease.
Triptonine B, a sesquiterpene pyridine alkaloid that isolated from Tripterygium hypoglaucum and Tripterygium wilfordii, inhibits HIV replication in H9 lymphocytes with an EC50 value of <0.10 μg/mL[1].
Cabotegravir is a potent HIV integrase inhibitor as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection. Cabotegravir is an inhibitor of OAT1 (IC50 0.81 μM) and OAT3 (IC50 0.41 μM).IC50 value: 0.81 μM (OAT1), 0.41 μM (OAT3) [1]Target: OAT1, OAT3Cabotegravir is a potent HIV integrase inhibitor in clinical development as an oral lead-in tablet and long-acting injectable for the treatment and prevention of HIV infection.[2] Cabotegravir is an HIV-1 integrase inhibitor under development as a tablet for both oral lead-in therapy and long-acting (LA) injectable for intramuscular dosing.[3]
GW433908 is a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, with improved solubility over the parent molecule and a potential for reduced pill burden on current dosing regimens; GW433908G is the calcium salt of the prodrug.IC50 Value:Target: HIV Proteasein vitro: There were no significant changes in buprenorphine or PI plasma levels and no significant changes in medication adverse effects or opioid withdrawal. Increased concentrations of the inactive metabolite buprenorphine-3-glucuronide suggested that darunavir-ritonavir and fosamprenavir-ritonavir induced glucuronidation of buprenorphine[1].in vivo: Fosamprenavir-ritonavir administered with methadone did not alter plasma amprenavir pharmacokinetics compared with historical control data; nor did it alter the unbound R-methadone at 2 and 6 hours after methadone dosing. Pharmacodynamic indexes remained essentially unchanged after adding fosamprenavir-ritonavir to methadone [2]. After a high-fat meal compared with fasting, (1) the bioavailability of GW433908G suspension was decreased by 20% and Cmax by 41%, and (2) for GW433908G tablets, there was no influence on AUC(12% lower Cmax). After a low-fat meal compared with fasting, (1) there was bioequivalence for GW433908G tablets, but (2) bioavailability was decreased by 23% for amprenavir capsules (Cmax was also lower, by 46%) [3].Clinical trial: Study of an Investigational Regimen Including FDA Approved HIV Drugs In HIV-Infected Pediatric Subjects. Phase 2
Atazanavir-d6 is deuterium labeled Atazanavir. Atazanavir (BMS-232632), a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration[1]. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp)[2]. Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM[3].
3'-Azido-3'-deoxy-5-methylcytidine (CS-92) is a potent xenotropic murine leukemia-related retrovirus (XMRV) inhibitor with a CC50 of 43.5 μM in MCF-7 cells. 3'-Azido-3'-deoxy-5-methylcytidine also inhibits HIV-1 reverse transcriptase with an EC50 of 0.06 μM in peripheral blood mononuclear (PBM) cells[1].
HIV-1 inhibitor-25 (compound R-12a) is a highly potent HIV-1 reverse transcriptase, with an IC50 value of 0.1061 μM. HIV-1 inhibitor-25 has high antiretroviral activity against WT HIV-1 with an EC50 of 13.6 nM, and exhibits relatively low cytotoxicity with a CC50 of 33.13 μM in MT-4 cells. HIV-1 inhibitor-25 also has inhibitory activity against HIV-1 mutant strains (L100I, K103N, Y181C, Y188L, E138K, F227L+V106A) with EC50 of 0.1961 ~ 5.8136 μM. HIV-1 inhibitor-25 can be used for researching AIDS[1].
Tenofovir alafenamide fumarate (GS-7340 fumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
PF-232798 is an orally active CCR5 antagonist with anti-HIV effects[1].
Influenza antiviral conjugate-1 (INT-2) is a HIV inhibitor, shows potent cell fusion inhibition[1].
HIV-1 inhibitor-60 (compound 45) is an HIV inhibitor with the potential for the research of infection diseases[1].
HIV-1 capsid inhibitor 1 is a potent HIV-1 Capsid inhibitor with an EC50 value of 3.13 µM. HIV-1 capsid inhibitor 1 shows antiviral activities[1].
BI-2540 is a HIV non-nucleoside reverse transcriptase (NNRT) inhibitor[1][2].
Raltegravir (MK 0518) sodium is a potent and orally active integrase (IN) inhibitor, used to treat HIV infection.
Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
L-Fd4A is an adenine derivative. L-Fd4A has anti-human immunodeficiency virus (HIV) (EC50=1.5 μM) and anti-hepatitis B virus (HBV) (EC50=1.7 μM) activity. L-Fd4A has low cytotoxicity[1].
Tenofovir alafenamide (GS-7340) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.
Apricitabine (SPD754; AVX754), the (-) enantiomer of 2′-deoxy-3′-oxa-4′-thiocytidine (dOTC), is a highly selective and orally active HIV-1 reverse transcriptase (RT) inhibitor (Ki=0.08 μM), as well as inhibits DNA polymerases α, β, and γ with Ki value of 300 μM, 12 μM, and 112.25 μM, respectively[1]. Apricitabine (SPD754; AVX754) shows promising antiretroviral efficacy, good tolerability and a low propensity for resistance selection in antiretroviral-naive HIV infection[2].
HIV-1 inhibitor-37 (Compound 83) is a potent HIV-1. HIV-1 inhibitor-37 has the potential for further development as novel latency reversing agents[1].
Corydine is a naturally occurring alkaloid which can be extracted from plants such as Croton echinocarpus leaves. Corydine is efficient on inhibiting reverse transcriptase (RT) activity with an IC50 of 356.8 μg/mL. Corydine displays significant in vitro anti-HIV potential, inhibiting 40% of the HIV-1 reverse transcriptase enzyme activity at a concentration of 450 μg/mL of Corydine[1].
Sodium copper chlorophyllin exerts antiviral activities against Influenza virus and HIV with IC50s of 50 to 100 μM for both of them.
HIV-1 inhibitor-23 (compound 12a) is a highly potent HIV-1 non-nucleoside reverse transcriptase inhibitor, with EC50s of 24.9 nM and 10.4 nM for HIV-1 WT and HIV-1 K103N, respectively. HIV-1 inhibitor-23 has low cytotoxicity (CC50 > 221 μM) and a favorable in vitro microsomal stability[1].
Wikstrol A is a potent antifungal, antimitotic and anti-HIV-1 Agent. Wikstrol A induces morphological deformation of P. oryzae mycelia with an MMDC value of 70.1 µM. Wikstrol A shows activity against microtubule polymerization with an IC50 value of 131 µM. Wikstrol A shows anti-HIV-1 activity with an IC50 value of 67.8 µM[1].
(+)-Dihydrocalanolide A (DHCal A; NSC 678323) is an orally active nonnucleoside inhibitor of Reverse Transcriptase. (+)-Dihydrocalanolide A can be used to HIV infection research[1].
Thiamine disulfide, a vitamin B1 derivative, is an oxidized dimer of Thiamine. Thiamine disulfide is a potent HIV-1 inhibitor. Thiamine disulfide significantly depresses HIV-1 transactivator (Tat) activity[1][2].
HIV-1 Rev (34-50) is a 17-aa peptide derived from the Rev-responsive element (RRE)-binding domains of Rev in HIV-1, with anti-HIV-1 activity.