Viramidine (taribavirin) / Sanofi - LARVOL DELTA

Implication of extrinsic and intrinsic apoptotic pathways in the targeted therapy of hepatocellular carcinoma using aptamer-labeled viramidine nanoparticles. (PubMed, BMC Cancer) - "The prepared VRM NPs labeled with APT could significantly elevate NO via activation of iNOS. In conclusion, APT-VRM NPs bioconjugate interferes with HCC cells through NO-mediated extrinsic and intrinsic apoptosis."

IO biomarker • Journal • Gastrointestinal Cancer • Hepatocellular Cancer • Oncology • Solid Tumor • BCL2 • CASP3 • CASP8 • CASP9 • CFLAR • FADD • TNFA

Contemporary and emerging pharmacotherapeutic agents for the treatment of Lassa viral haemorrhagic fever disease. (PubMed, J Antimicrob Chemother) - "There are, however, off-label therapeutics being used (ribavirin and convalescent plasma) whose efficacy is suboptimal...Considered therapeutic options include favipiravir, taribavirin, Arevirumab-3 and experimental drugs such as losmapimod, adamantyl diphenyl piperazine 3.3, Arbidol (umifenovir) and decanoyl-RRLL-chloromethyl ketone (dec-RRLL-CMK). Current treatments for LF are limited, hence the institution of mitigating measures to prevent infection is of utmost importance and should be prioritized, especially in endemic regions. Heightened searches for other therapeutic options with greater efficacy and lower toxicity are still ongoing, as well as for vaccines as the absence of these classifies the disease as a priority disease of high public health impact."

Journal • Infectious Disease

AZT acts as an anti-influenza nucleotide triphosphate targeting the catalytic site of A/PR/8/34/H1N1 RNA dependent RNA polymerase. (PubMed, J Comput Aided Mol Des) - "To develop potent drugs that inhibit the activity of influenza virus RNA dependent RNA polymerase (RdRp), a set of compounds favipiravir, T-705, T-1105 and T-1106, ribavirin, ribavirin triphosphate viramidine, 2FdGTP (2'-deoxy-2'-fluoroguanosine triphosphate) and AZT-TP (3'-Azido-3'-deoxy-thymidine-5'-triphosphate) were docked with a homology model of IAV RdRp from the A/PR/8/34/H1N1 strain. Overall, our computational results in correlation with experimental studies gives information for the first time about the binding modes of the known influenza antiviral compounds in different models of vRNA replication by IAV RdRp. This in turn gives new structural insights for the development of new therapeutics exhibiting high specificity to the PB1 catalytic site of influenza A viruses."

Journal • Infectious Disease

Taribavirin and 5-Fluorouracil-Loaded Pegylated-Lipid Nanoparticle Synthesis, p38 Docking, and Antiproliferative Effects on MCF-7 Breast Cancer. (PubMed, Pharm Res) - "The effect of TBV nanoparticles on MCF-7 cells may be due to its inhibitory effect against p38MAPK protein, where it fits inside the active pocket site of the p38 protein molecular surface, with a minimum binding affinity of -5.5 kcal/mol (rmsd of 1.07), and it formed strong hydrogen bonds with amino acids ASP'168, ILE'166, HIS'148, and ILE'147. Further studies are warranted to investigate the mechanistic details of the proposed approach."

Journal • Biosimilar • Breast Cancer • Oncology • Solid Tumor

Viramidine-Loaded Galactosylated Nanoparticles Induce Hepatic Cancer Cell Apoptosis and Inhibit Angiogenesis. (PubMed, Appl Biochem Biotechnol) - "Ribavirin, an antiviral nucleoside inhibitor, accumulates inside red blood cells, causing anemia...Here, viramidine, 5-fluorouracil, and paclitaxel-loaded Gal-SLN were characterized inside cells...Gal-SLN application on breast cancer MCF-7 cells confirmed its specificity against liver cancer HepG2 cells. We conclude that viramidine-encapsulated Gal-SLN has anticancer and anti-angiogenic activities against hepatocarcinoma."

Journal

Enzyme kinetic assays validate fragment inhibitors of Trichomonas vaginalis nucleoside ribohydrolase enzymes (ACS-Sp 2020) - "Viramidine was determined to be the most potent inhibitor of AGNH with a KI value of 240 nM. The phenylpyridine fragment hit derivative 3-(4-methylpyridin-3-yl)phenol was determined to be the most potent inhibitor of UNH with a KI value of 3 μM."