antiretroviral

Stavudine (BMY-27857), a nucleoside reverse transcriptase inhibitor analog of thymidine, has activity against HIV.

Didanosine (ddI) is a nucleoside reverse transcriptase inhibitor analog of adenosine (IC50: 0.49 μM).

Cabotegravir (S/GSK1265744) (GSK744, GSK1265744) is a long-acting HIV integrase inhibitor and inhibits the HIV-1 integrase catalyzed strand transfer reaction (IC50: 3.0 nM).

Lenacapavir (GS-6207) is the first HIV-1 capsid inhibitor approved by the U.S. Food and Drug Administration, the European Medicines Agency, and Health Canada for the treatment of MDR HIV-1 infection.[3]

Dexelvucitabine (RVT), a nucleoside reverse transcriptase inhibitor, is used potentially for the treatment of HIV infection.

AG 555 (Tyrphostin B46) is an EGFR tyrosine kinase inhibitor.

Hck-IN-1 is a selective Nef-dependent Hck inhibitor (IC50s: 2.8 μM and >20 μM for Nef:Hck complex and Hck) with antiretroviral activity. Hck-IN-1 is a direct and wide HIV-1 Nef antagonist with an IC50 of 100-300 nM for wild-type HIV-1 replication.

Apricitabine (SPD754) is a highly selective and orally active HIV-1 reverse transcriptase inhibitor (Ki=0.08 μM), the (-) enantiomer of 2′-deoxy-3′-oxy-4′-thiocytidine (dOTC) . Apricitabine inhibits DNA polymerase α, β and γ with Ki values of 300 μM, 12 μM and 112.25 μM, respectively. Apricitabine has shown good antiretroviral therapeutic efficacy in antiretroviral HIV-infected patients, with good tolerability and low selective resistance.

Ancriviroc (SCH-351125) is an oxime-piperidine compound with strong antiretroviral activity and an orally bioavailable small molecule chemokine receptor CCR5 antagonist (Kd value 9.27nM) that enters HIV-1 through the CCR5 co-receptor and is used to study HIV-1.

DNA polymerase-IN-1, a DNA polymerase inhibitor, exhibited antiproliferative activity against tumor cells with a half-inhibitory concentration (IC50) of 20.7 μM. DNA polymerase-IN-1 inhibited Taq DNA polymerase with an IC50 of less than 250 μM. DNA polymerase-IN-1 was shown to inhibit Taq DNA polymerase by RT- DNA polymerase-IN-1 showed antiretroviral activity in vitro by RT-PCR assay and can be used to study oxidative damage and colorectal cancer.

Nevirapine (NVP) is a benzodiazepine non-nucleoside reverse transcriptase inhibitor. In combination with other antiretroviral drugs, nevirapine reduces HIV viral loads and increases CD4 counts, thereby retarding or preventing the damage to the immune system and reducing the risk of developing AIDS.

Tenofovir alafenamide (GS-7340) is a nucleotide reverse transcriptase inhibitor (NRTI) and a novel ester prodrug of the antiretroviral tenofovir.

Bavtavirine is a potent non-nucleoside reverse transcriptase inhibitor (NNRTIs) that inhibits HIV replication by inhibiting HIV-1 reverse transcriptase activity and preventing the transcription of viral RNA into DNA for use in Highly Active Antiretroviral Therapy (HAART) programs and HIV disease studies

Tipranavir C-14 is an antiretroviral protease inhibitor primarily used for the treatment and prevention of human immunodeficiency virus (HIV) infection and acquired immunodeficiency syndrome (AIDS).

Lenacapavir, also known as GS-6207, is an HIV-1 capsid inhibitor. It demonstrates an average EC50 of 50 pM (ranging from 20-160 pM) against 23 clinical isolates of HIV-1 from diverse subtypes, with tests performed in peripheral blood mononuclear cells (PBMCs). In vitro, Lenacapavir exhibits picomolar potency and shows no cross-resistance with existing antiretroviral compounds. Furthermore, Lenacapavir displays significant antiviral activity in individuals with HIV-1, regardless of prior treatment history, with no pre-existing resistance detected.

(S)-Batylalcohol (1-O-Octadecyl-sn-glycerol) is an analogue of phosphonoformic acid (PFA) and demonstrates higher in vitro antiviral activity against human immunodeficiency virus type 1 (HIV-1) compared to PFA. This compound is applicable in antiretroviral research.

SB 203580 hydrochloride (Adezmapimod hydrochloride) is a selective, ATP-competitive p38 MAPK inhibitor that induces mitochondrial autophagy and cytosolic autophagy and inhibits SAPK2a/p38, SAPK2b/p38β2, LCK, GSK3β, and PKBα. SB 203580 hydrochloride has been shown to be useful in antiretroviral therapy. 203580 hydrochloride inhibits amphoteric mechanical anomalous pain in a mouse model of antiretroviral-induced neuropathic pain.

Stampidine can prevent the sexual transmission of HIV-1. It exhibited remarkable subnanomolar to low nanomolar in vitro antiretroviral potency against nucleoside reverse transcriptase inhibitor-resistant primary clinical HIV isolates, non-nucleoside RT-re

Indinavir, threo- is a protease inhibitor utilized as a component of highly active antiretroviral treatment to HIV/AIDS.

Betulinic acid (ALS-357) is a pentacyclic lupane-type triterpene derivative of betulin (isolated from the bark of Betula alba, the common white birch) which has antiretroviral, antimalarial, and anti-inflammatory properties, as well as a more recently discovered potential as an anticancer agent, by inhibition of topoisomerase.

Tenofovir exalidex (CMX 157) is a lipid-conjugated acyclic nucleotide analog of Tenofovir, demonstrating efficacy against wild-type and antiretroviral-resistant HIV strains, including those resistant to multiple nucleoside/nucleotide analogs. It effectively inhibits all major HIV-1 and HIV-2 subtypes in fresh human PBMCs, as well as all evaluated HIV-1 strains in monocyte-derived macrophages, displaying EC50 values between 0.2 and 7.2 nM. Oral administration of CMX157 shows no apparent toxicity. Additionally, Tenofovir exalidex exhibits antiviral properties against HBV.

AZT triphosphate TFA (3'-Azido-3'-deoxythymidine-5'-triphosphate TFA) is a active triphosphate metabolite of Zidovudine (AZT). AZT triphosphate TFA exhibits antiretroviral activity and inhibits replication of HIV. AZT triphosphate TFA also inhibits the DNA polymerase of HBV. AZT triphosphate TFA activates the mitochondria-mediated apoptosis pathway[1][2][3]. Treatment with 100 μM Zidovudine (AZT) for 48h disrupts the mitochondrial tubular network via accumulation of AZT triphosphate (AZT-TP) in H9c2 cells. AZT triphosphate accumulation causes downregulation of Opa1 and upregulation of Drp1. AZT triphosphate causes mitochondrial dysfunction, increases the production of cytotoxic reactive oxygen species (ROS), and impairs the balance of the mitochondrial quality control system in H9c2 cell model established from rat embryonic myoblasts[1]. [1]. Ryosuke Nomura, et al. Azidothymidine-triphosphate Impairs Mitochondrial Dynamics by Disrupting the Quality Control System. Redox Biol. 2017 Oct;13:407-417. [2]. Takeya Sato, et al. Engineered Human tmpk/AZT as a Novel Enzyme/Prodrug Axis for Suicide Gene Therapy. Mol Ther. 2007 May;15(5):962-70. [3]. K Y Hostetler, et al. Enhanced Oral Absorption and Antiviral Activity of 1-O-octadecyl-sn-glycero-3-phospho-acyclovir and Related Compounds in Hepatitis B Virus Infection, in Vitro. Biochem Pharmacol. 1997 Jun 15;53(12):1815-22.

Fosamprenavir (Amprenavir phosphate; GW 433908) is a phosphate ester prodrug of the antiretroviral protease inhibitor Amprenavir, offering improved solubility over the parent molecule and exhibiting anti-HIV infection effects [1].

Indinavir is an orally administered, specific HIV protease inhibitor commonly used in combination therapy as part of highly active antiretroviral therapy (HAART) for HIV/AIDS. Indinavir also inhibits the activation of MMP-2 in endothelial cells and exhibits affinity for α7-nAchR and SARS-CoV-2 Mpro.