Famciclovir(BRL 42810) is a guanine analogue antiviral drug used for the treatment of various herpesvirus infections.IC50 Value: Refer to penciclovirTarget: HSVFamciclovir is the diacetyl 6-deoxy analog of the active antiviral compound penciclovir with potential use in the treatment of infections caused by the herpes family of viruses [1]. Famciclovir, a synthetic acyclic guanine derivative, is a prodrug which, after oral administration, is rapidly metabolised to the highly bioavailable antiviral compound penciclovir [2].in vitro: Famciclovir induced rapid, dose-dependent suppression of viral replication and reduction in alanine aminotransferase (ALT), with greatest efficacy in the 500-mg tid treatment group. HBV DNA reduction was maintained throughout the treatment period. ALT also steadily declined during the treatment period [3]. in vivo: In rat, following dosing at 40 mg/kg, famciclovir was rapidly and extensively metabolized to the active antiviral compound penciclovir, which reached peak concentrations in the plasma (mean 3.5 micrograms/ml) at 0.5 h [4]. Necrotic hepatitis was significantly (p < 0.01) reduced by treatment with FCV, VACV and ACV at a dose of 50 mg/kg per day divided into 3 doses. No significant effect was achieved with BVDU at 200 mg/kg per day. Treatment with FCV at 50 mg/kg per day, ACV at 100 mg/kg per day, and VACV at 200 mg/kg per day significantly (p < 0.001) decreased mortality in mice [5].Clinical trial: Famciclovir Pediatric Formulation In Children 1 to 12 Years Of Age With Herpes Simplex Infection. Phage3
Tromantadine hydrochloride, an Amantadine derivative with antiherpetic activity, inhibits herpes simplex virus type 1 (HSV-1) and HSV-2 replication[1].
HSV-1 Protease substrate is a peptide substrate for HSV-1 (Herpes Simplex Virus Type 1) protease, and the specificity constant (kcat/Km) at pH 7.5 for cleavage is 5.2 M-1 s-1[1].
Surfen dihydrochloride is a potent HS (heparan sulfate) antagonist. Surfen binds to glycosaminoglycans. Surfen neutralizes the anticoagulant activity of both unfractionated and low molecular weight heparins. Surfen affects sulfation of heparin and inhibits degradation by heparin lyases. Surfen inhibits FGF2 binding and signaling. Surfen inhibits cell attachment, and virus infection[1].
5-Hydroxymethyl-2'-deoxyuridine is a nucleoside analog. 5-Hydroxymethyl-2'-deoxyuridine inhibits the replication of multiple human leukemia cell lines with IC50 values of 1.7-5.8 μM. 5-Hydroxymethyl-2'-deoxyuridine prolongs the survival of mice carrying L1210 leukemia. 5-Hydroxymethyl-2'-deoxyuridine can be used for the research of cell replication and leukemia[1][2][3].
Epipodophyllotoxin acetate (4-O-Epipodophyllotoxinyl acetate; compound 4) is a cyclolignan that exhibits antineoplastic and antiviral activities. Epipodophyllotoxin acetate inhibits HSV and VSV, with IC50s of 0.2 and 0.1 μg/mL, respectively[1].
Valomaciclovir stearate (ABT 606), a nucleoside analog, is the Omaciclovir (HY-116174) prodrug. Valomaciclovir stearate has antiviral activity against HSV-1 and varicella zoster virus (VZV)[1].
Valacyclovir-d4 hydrochloride is the deuterium labeled Valacyclovir hydrochloride. Valacyclovir hydrochloride (Valaciclovir hydrochloride) is an orally active antiviral drug for herpes simplex, herpes zoster, and herpes B. Valacyclovir hydrochloride inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir hydrochloride is a prodrug of Aciclovir (HY-17422)[1][2][3][4][5].
Fiacitabine(NSC 382097; FIAC; FOAC) is a selective inhibitior of DNA replication of herpes simplex virus(HSV) with IC50 values of 2.5 nM and 12.6 nM for HSV1 and HSV2, respectively. IC50 value: 2.5/12.6 nM (HSV1/2) [2]Target: HSVFIAC suppressed by 90% the replication of various strains of herpes simplex virus types 1 and 2 at concentrations of 0.0025 to 0.0126 microM. Cytotoxicity was minimal, as determined by trypan blue dye exclusion with norman Vero, WI-38, and NC-37 cell proliferation; the 50% inhibitory dose was 4 to 10 microM in a 4-day assay. FIAC was active at much lower concentrations than arabinosylcytosine, iododeoxyuridine, and arabinosyladenine. It was slightly more active against herpes simplex virus type 1 than acycloquanosine and slightly more toxic to normal cells. FIAC was about 8,000 times more active against the replication of wild-type herpes simplex virus type 1 than against a mutant strain lacking the expression of virus-specified thymidine kinase [2].
2-Deoxy-D-glucose-13C-1 is the 13C labeled 2-Deoxy-D-glucose. 2-Deoxy-D-glucose is a glucose analog that acts as a competitive inhibitor of glucose metabolism, inhibiting glycolysis via its actions on hexokinase[1][2].
CMX001 (Brincidofovir; HDP-CDV) was developed as an orally active, lipophilic form of cidofovir (CDV); has enhanced activity in vitro and in vivo compared to CDV against certain herpesviruses, adenoviruses and orthopoxviruses.IC50 Value: 5.5 nM (EC50, in PDA at 7 dpi) [3]Target: anti-CMVCMX001 is currently in Phase II clinical studies for development as a therapeutic agent for human CMV, adenovirus and BK virus infections, as well as, for adverse events following smallpox vaccinations.in vitro: In PDA at 7 dpi, the CMX001 50% effective concentration (EC50) was 5.55 nM, the 50% cytotoxic concentration (CC50) was 184.6 nM, and the 50% selectivity index (SI50) was 33.3. The EC90 was 19.7 nM, the CC90 was 5,054 nM, and the SI90 was 256.1. In COS-7 cells, JCV replication was faster and the EC50 and EC90 were 18- and 37-fold higher than those in PDA, i.e., 0.1 μM and 0.74 μM (CC50, 0.67 μM; SI50, 6.7; CC90, 12.2 μM; SI90, 16.5) at 5 dpi [3].in vivo: CMX001 and CDV are equally efficacious at protecting mice from mortality following high ectromelia virus doses (10,000 x LD(50)) introduced by the intra-nasal route or small particle aerosol. Using CMX001 at a 10mg/kg dose followed by 2.5mg/kg doses every other-day for 14 days provided solid protection against mortality and weight loss following an intra-nasal challenge of (100-200) x LD(50) of ectromelia virus [1]. When CMX001 was administered orally to mice infected with HSV-1, mortality was reduced significantly (p≤0.001) with all three dose levels when treatments were initiated 24 h post viral inoculation. When treatments were started 48 h post viral inoculation, 5 and 2.5 mg/kg significantly reduced mortality (p≤ 0.001). If treatments were delayed until 72 h post viral inoculation, CMX001 did not reduce mortality or increase the mean day to death. When mice were infected intranasally with HSV-1 and treatments initiated 24 h post viral inoculation using CMX001 at 5 mg/kg or ACV at 100 mg/kg, virus replication in target organs was reduced by both CMX001 and ACV when compared to vehicle treated mice [2]. Toxicity: Diarrhea was the most common adverse event in patients receiving CMX001 at doses of 200 mg weekly or higher and was dose-limiting at 200 mg twice weekly. Myelosuppression and nephrotoxicity were not observed [4].
FK-3000 is a potent anti-tumor agent that inhibits the growth of carcinoma cells through apoptosis and induction cell cycle arrest. FK-3000 also exhibit antiviral effects against HSV-1 and HIV-1[1][2][3][4].
5-Nitrobarbituric acid is a herpes simplex virus type-1 (HSV-1) inhibitor (IC50=1.7 μM)[1].
Ganciclovir (INN) is an antiviral medication used to treat or prevent cytomegalovirus (CMV) infections. Ganciclovir is a synthetic analogue of 2′-deoxy-guanosine. It is first phosphorylated to ganciclovir monophosphate by a viral kinase encoded by the cytomegalovirus (CMV) gene UL97 during infection. Subsequently, cellular kinases catalyze the formation of ganciclovir diphosphate and ganciclovir triphosphate, which is present in 10-fold greater concentrations in CMV or herpes simplex virus (HSV)-infected cells than uninfected cells. A prodrug form with improved oral bioavailability (valganciclovir) has also been developed.
Stearyl gallate is an alkyl gallate with a long alkyl chain (carbon number of 18). Stearyl gallate has an antioxidant activity, and a weak antiviral activity against HSV-1[1][2].
HSV-1/HSV-2-IN-1 (compound 7d) is a HSV-1 and HSV-2 inhibitor, with EC50s of 7.6, 7.6, 4, and 12 μM for HSV-1 (KOS), HSV-2 (G), HSV-1 TK- KOS ACVr and vaccinia virus in human embryonic lung fibroblast cell cultures[1].
Penciclovir (VSA 671) sodium is a potent and selective anti-herpesvirus agent with EC50 values of 0.5, 0.8 µg/ml for HSV-1 (HFEM), HSV-2 (MS), respectively. Penciclovir sodium shows anti-herpesvirus activity with no-toxic. Penciclovir sodium preventes mortality in mouse[1][2].
Galactofucan (Fucogalactan) is a sulfated polysaccharide. Galactofucan can be extracted from brown seaweed Saccharina longicruris with anticoagulant, anti-tumor, anti-thrombosis, anti-inflammatory and antiviral properties. Galactofucan shows antiviral activities to HSV-1 and HSV-2 with IC50s of 0.76 and 1.34 µg/mL, respectively. Galactofucan can be used for the research of cancer and inflammation[1][2].
Surfactin is a potent cyclic lipopeptide biosurfactants that mediates flux of mono-and divalent cations, such as calcium, across lipid bilayer membranes. Surfactin can act as an antimicrobial adjuvant with anti-bacterial, anti-fungal, antimycoplasma and hemolytic effects[1][2]. Surfactin also has antiviral activity against a variety of enveloped viruses[3].
Leachianone G is an antiviral flavonoid from the root bark of Morus alba L. Leachianone G shows potent antiviral activity against herpes simplex type 1 virus (HSV-1) with an IC50 value of 1.6 μg/mL[1].
Zerumbone is a monocyclic sesquiterpene compound isolated from the rhizomes of Zingiber zerumbet Smith. Zerumbone potently inhibits the activation of Epstein-Barr virus with an IC50 of 0.14 mM. Zerumbone has anti-cancer, antioxidant, anti-inflammatory and anti-proliferative activity[1][2].
HSV-TK substrate is a substrate for HSV-TK, and induces multi-log cytotoxicity in HSV-TK-expressing and bystander cells. HSV-TK substrate shows antitumor activity[1].
Pritelivir mesylate hydrate (BAY 57-1293 mesylate hydrate), an inhibitor of the viral helicase-primase complex, exhibits antiviral activity in vitro and in animal models of herpes simplex virus (HSV) infection. Pritelivir mesylate hydrate is active against herpes simplex virus types 1 and 2 (HSV-1 and HSV-2) with the IC50 of 0.02 μM against HSV1-2[1].
Valacyclovir hydrochloride hydrate is a potent antiviral agent. Valacyclovir hydrochloride hydrate can be used in the management of herpes simplex, herpes zoster and herpes B. Valacyclovir hydrochloride hydrate can be formulate ocular inserts for the treatment of ocular herpes. Valacyclovir hydrochloride hydrate is a prodrug and can be rapidly converted into acyclovir in vivo[1][2].
Cangorinine E-1 (compound 11) is a dihydroagarofuran derivative of the sesquiterpenoid family. Cangorinine E-1 exhibits weak inhibitory effects on herpes simplex virus type II (HSV)[1].
Omaciclovir (H2G) is a potent and selective inhibitor of herpesvirus replication. Omaciclovir is a nucleoside analog with antiviral activity[1].
Cyclopropavir (Filociclovir; ZSM-I-62; MBX-400) is a broad-spectrum anti-herpesvirus compound, has good antiviral activity against cytomegalovirus (CMV), herpes simplex virus (HHV)-6 and HHV-8 with EC50s of 0.7 μM to 8 μM[1].
Imiquimod-d9 is deuterium labeled Imiquimod. Imiquimod (R 837), an immune response modifier, is a selective toll like receptor 7 (TLR7) agonist. Imiquimod exhibits antiviral and antitumor effects in vivo. Imiquimod can be used for the research of external genital, perianal warts, cancer and COVID-19[1][2].
GLR-19 is an anti-HIV peptide. GLR-19 also has antiviral activity against HSV-2[1][2].
LDC4297 hydrochloride is a selective inhibitor of CDK7 with an IC50 value of 0.13 nM. LDC4297 hydrochloride inhibits human cytomegalovirus (HCMV) replication with an EC50 value of 24.5 nM. LDC4297 hydrochloride shows broad antiviral activities to Herpesviridae, Adenoviridae, Poxviridae, Retroviridae and Orthomyxoviridae with EC50 values of 0.02-1.21 μM. LDC4297 hydrochloride can be used for the research of infection[1].