lamivudine / Generic mfg. 
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  • ||||||||||  Zontivity (vorapaxar) / Merck (MSD)
    Journal:  Enantioselective synthesis of a chiral intermediate of himbacine analogs by Burkholderia cepacia lipase A. (Pubmed Central) -  Jul 29, 2021   
    The enantiomers of (4R/S)-4-hydroxy-N, N-diphenyl-2-pentynamide are key chiral synthons for the synthesis of thrombin receptor antagonists such as vorapaxar...Using the optimize conditions, (4R)-4-hydroxy-N, N-diphenyl-2-pentynamide with 94.5% ee value and 48.93% conversion ratio was achieved. Our investigation on this lipase reveals lipase A as a promising biocatalyst for producing chiral propargyl alcohol for preparation of novel himbacine analogs.
  • ||||||||||  lamivudine HBV / Generic mfg.
    Journal:  Synthesis and evaluation of new phenyl acrylamide derivatives as potent non-nucleoside anti-HBV agents. (Pubmed Central) -  Jul 28, 2021   
    Among them, compound 4Bs could potently inhibit HBV DNA replication in wild-type and lamivudine (3TC)/entecavir resistant HBV mutant strains with IC values of 0.19 and 0.18 μM, respectively...Molecular docking study revealed that 4Bs could fit well into the dimer-dimer interface of HBV core protein by hydrophobic, π-π and H-bond interactions. Considering the potent anti-HBV activity, low toxicity and diverse anti-HBV mechanism from that of nucleoside anti-HBV agent 3TC, compound 4Bs might be a promising lead to develop novel non-nucleoside anti-HBV therapeutic agents, and warranted further investigation.
  • ||||||||||  lamivudine HBV / Generic mfg.
    Clinical, Journal:  Prevention and treatment of new hepatitis B after living donor liver transplantation in children. (Pubmed Central) -  Jul 28, 2021   
    After their operations, the children were given lamivudine for anti-hepatitis B virus (HBV) treatment, a hepatitis B vaccine or intermittent supplements of hepatitis B immunoglobulins to prevent recurrence of the infection, and entecavir for anti-hepatitis B treatment...The long-term prophylactic therapy of nucleoside analogues combined with hepatitis B immunoglobulins should be used for a long time after liver transplantation with a liver positive for HBcAg. Discontinuation of nucleoside analogues is associated with a higher risk of the new onset of hepatitis B. Entecavir has a significant effect on the treatment of postoperative new hepatitis B in children.
  • ||||||||||  levofloxacin / Generic mfg., lamivudine / Generic mfg.
    Journal:  Probing the degradation of pharmaceuticals in urine using MFC and studying their removal efficiency by UPLC-MS/MS. (Pubmed Central) -  Jul 20, 2021   
    The voltage curve obtained showed that the presence of pharmaceuticals had an initial negative impact on power generation along with increased organic content; however, after the reactor acclimatization, increased power output was achieved with maximum organics removal at 30 h of retention time. This work opens a new perspective for the anoxic biodegradation of pharmaceuticals and can be useful in future bioremediation studies.
  • ||||||||||  lamivudine HBV / Generic mfg.
    Preclinical, Journal:  A long-acting 3TC ProTide nanoformulation suppresses HBV replication in humanized mice. (Pubmed Central) -  Jul 17, 2021   
    To this end, we modified lamivudine (3TC), a nucleoside analog inhibitor of both viruses, into a lipophilic monophosphorylated prodrug (M23TC)...A single intramuscular dose of 75mg/kg 3TC equivalents of nanoformulated NM23TC provided sustained drug levels and suppressed HBV replication in humanized mice for 4weeks. The results support further development of this long-acting 3TC nanoformulation for HBV treatment and prevention.
  • ||||||||||  lamivudine HBV / Generic mfg.
    Clinical, Journal:  Management of Hepatitis-B Virus Infection in Immunocompromised Children. A Single Center Experience. (Pubmed Central) -  Jul 11, 2021   
    There is a residual risk of acute hepatitis B in immunocompromised children, mortality rate was substantial, potentially related to the delays in commencing chemotherapy caused by liver dysfunction. Tenofovir-DF or entecavir are the drugs of choice for HBV treatment in immunocompromised children.
  • ||||||||||  lamivudine HBV / Generic mfg.
    Journal:  Synthesis and Bioactivity of N-(4-Chlorophenyl)-4-Methoxy-3-(Methylamino) Benzamide as a Potential Anti-HBV Agent. (Pubmed Central) -  Jul 9, 2021   
    Our results show that IMB-0523 has higher anti-HBV activity in both wild-type HBV (IC: 1.99 µM) and drug-resistant HBV (IC: 3.30 µM) than lamivudine (3TC, IC: 7.37 µM in wild-type HBV, IC: >440 µM in drug-resistant HBV)...Further, IMB-0523 showed potent anti-HBV activity in DHBV-infected ducks. Thus, IMB-0523 may be a potential anti-HBV agent with different mechanisms than current anti-HBV treatment options.
  • ||||||||||  undisclosed HBV therapeutic / Kainos Medicine, Institut Pasteur Korea
    Journal:  A new high-content screening assay of the entire hepatitis B virus life cycle identifies novel antivirals. (Pubmed Central) -  Jul 6, 2021   
    Patient-derived HBV genotype C was efficiently inhibited by fludarabine (EC 0.08 μM) and dexmedetomidine (EC 8.7 μM)...We used this system to screen drug libraries and identified novel anti-HBV inhibitors that potently inhibit HBV in various phases of its life cycle. This assay will be an important new tool to study the HBV life cycle and accelerate the development of novel therapeutic strategies.
  • ||||||||||  zidovudine / Generic mfg., lamivudine HBV / Generic mfg.
    Journal:  Structural dynamics and susceptibility of anti-HIV drugs against HBV reverse transcriptase. (Pubmed Central) -  Jul 4, 2021   
    In the present study, we aimed to investigate the structural dynamics and susceptibility of the known anti-HIV drugs (stavudine [d4T], didanosine [DDI], and zidovudine [ZDV]) against HBV-RT enzyme in comparison to the anti-HBV drug lamivudine (3TC) and deoxythymidine triphosphate (dTTP) substrate using several computational approaches...The predicted binding free energy results based on QM/MM-GBSA and MM/GB(PB)SA methods suggested that the susceptibility towards HBV-RT of d4T and ZDV is higher than that of 3TC and dTTP. Altogether, this work sheds light on the potentiality of d4T and ZDV as a promising drug for HBV-infected patients harboring 3TC resistance.Communicated by Ramaswamy H. Sarma.
  • ||||||||||  lamivudine / Generic mfg.
    Journal:  To dose-adjust or not to dose-adjust: 3TC dose in kidney impairment. (Pubmed Central) -  Jun 30, 2021   
    Because 3TC is a well-tolerated drug with a wide therapeutic window, dose adjustment may be unnecessary among PLWH with eGFR between ≥30 and ≤49 ml/min/1.73m2. Clinical judgement is key when weighing the risks and benefits of 3TC dose adjustment for PLWH experiencing gastrointestinal symptoms or moderate lab abnormalities.
  • ||||||||||  Vemlidy (tenofovir alafenamide) / Gilead
    Journal:  Nucleos(t)ide analogue therapy: The role of tenofovir alafenamide. (Pubmed Central) -  Jun 30, 2021   
    ETV may be less effective in patients with lamivudine-resistant strains, and TDF is associated with impaired renal function and reductions in bone mineral density...The main limitation to prescribing TAF is its price. The European Association for the Study of the Liver has suggested selecting TAF or ETV instead of TDF in patients >65 years old and in those with a risk of osteoporosis or renal abnormalities, and to prescribe TAF rather than ETV in patients previously exposed to NAs.
  • ||||||||||  Clinical, Journal:  Characteristics of drug resistance in HIV-1 CRF55_01B from ART-experienced patients in Guangdong, China. (Pubmed Central) -  Jun 26, 2021   
    The European Association for the Study of the Liver has suggested selecting TAF or ETV instead of TDF in patients >65 years old and in those with a risk of osteoporosis or renal abnormalities, and to prescribe TAF rather than ETV in patients previously exposed to NAs. High frequencies of DRMs and resistance were observed among CRF55_01B-infected patients failing ART in Guangdong, and interventions may be considered to minimize ecological contributions to ART.
  • ||||||||||  lamivudine HBV / Generic mfg.
    Clinical, Journal:  Rapid Turnover of HBV cccDNA Indicated by Monitoring Emergence and Reversion of Signature-Mutation in Treated Chronic Hepatitis B Patients. (Pubmed Central) -  Jun 22, 2021   
    Similarly, in lamivudine-resistant patients who switched to interferon therapy, serum HBV RNA population bearing 100% LAM mutations fully reversed back to wild type within 24~48 weeks. The genetic composition dynamics of serum HBV RNA and biopsy cccDNA in treated HBV patients indicates that cccDNA turnover occurs relatively rapidly (several months), offering a possibility of HBV cure with finite therapy through completely blocking cccDNA replenishment.
  • ||||||||||  ATI-2173 / Antios Therap
    Journal:  ATI-2173, A Novel Liver-Targeted Non-Chain Terminating Nucleotide for HBV Cure Regimens. (Pubmed Central) -  Jun 22, 2021   
    ATI-2173 activity was decreased by viral polymerase mutations associated with entecavir, lamivudine, and adefovir resistance, but not capsid inhibitor resistance mutations...Despite reduced plasma clevudine exposure, liver concentrations of the 5'-triphosphate were equivalent following ATI-2173 versus clevudine administration. By selectively delivering the 5'-monophosphate to the liver, while retaining the unique anti-HBV activity of the 5'-triphosphate, ATI-2173 may provide an improved pharmacokinetic profile for clinical use, reducing systemic exposure of clevudine and potentially eliminating skeletal myopathy.
  • ||||||||||  lamivudine / Generic mfg.
    Preclinical, Journal:  Reverse Transcriptase Affects Gametogenesis and Preimplantation Development in Mouse. (Pubmed Central) -  Jun 22, 2021   
    By selectively delivering the 5'-monophosphate to the liver, while retaining the unique anti-HBV activity of the 5'-triphosphate, ATI-2173 may provide an improved pharmacokinetic profile for clinical use, reducing systemic exposure of clevudine and potentially eliminating skeletal myopathy. The administration of lamivudine affected the processes of spermatogenesis and oogenesis as well as the in vitro preimplantation development of mouse embryos.
  • ||||||||||  lamivudine HBV / Generic mfg.
    Review, Journal:  Nucleos(t)ide analogues and Hepatitis B virus-related hepatocellular carcinoma: A literature review. (Pubmed Central) -  Jun 5, 2021   
    In this review, we have discussed the different classes of nucleos(t)ide analogues used in the treatment of Hepatitis B virus and their relationship with the development of hepatocellular carcinoma. Furthermore, we discussed the effect of treatment of Hepatitis B virus with Nucleoside analogues (NAs) before, during and after surgery, chemoembolization, radiofrequency ablation, and chemotherapy for the treatment of hepatocellular carcinoma.
  • ||||||||||  zidovudine / Generic mfg.
    [VIRTUAL] MEASLES PNEUMONIA IN AN IMMUNOCOMPROMISED CHILD () -  Jun 2, 2021 - Abstract #ESPID2021ESPID_1223;    
    On the 6th day of in-patient treatment, the girl was transferred to the infectious department, on the 13 th day she was discharged home (received antiretroviral therapy, cefixime, co-trimoxazole)...Measles pneumonia in immunocompromised HIV-infected patients has viral-bacterial etiology and requires aggressive combination of antibiotic therapy in combination with enhanced antiretroviral therapy. Protective immunity against measles has been studied but still not fully understood for HIV-infected patients.
  • ||||||||||  lamivudine HBV / Generic mfg.
    [VIRTUAL] Molecular diversity of hepatitis B virus in HIV infected patients at Mbagathi District Hospital, Nairobi () -  May 27, 2021 - Abstract #IASHIV2021IAS_HIV_1288;    
    However, growth deficits persisted for CPHIV regardless of IPA exposure type and for CHEU without any IPA exposure highlighting the need for continued vigilance and interventions in these subgroups to support achievement of their growth potential. Inadequate HBV co-management in HIV-HBV co-infected patients is likely to lead to the emergence and circulation of HBV escape mutants of interest to public health management and there may be high HBV drug resistance strains to available ART options in Kenya among HIV patients.
  • ||||||||||  [VIRTUAL] HIV minority resistance variants partially explain genotypic-phenotypic discordance () -  May 27, 2021 - Abstract #IASHIV2021IAS_HIV_995;    
    Discordance, mostly represented by genotypic DR overestimation, was partially explained by NGS minority DR variants. This suggests that minority DR variants might help refine genotypic interpretation algorithms to avoid inappropriate choice of drugs; but also, existence of alternative explanations.
  • ||||||||||  doravirine/islatravir (MK-8591A) / Merck (MSD)
    [VIRTUAL] Week 96 metabolic and bone outcomes of a Phase 2b trial of islatravir and doravirine () -  May 27, 2021 - Abstract #IASHIV2021IAS_HIV_958;    
    No unexpected or concerning metabolic or bone effects were observed in treatment-naive adults living with HIV-1 receiving ISL+DOR. Due to small sample size in this trial, clinical significance will be further investigated in phase 3 clinical studies.