Preferred Label : Tenofovir Alafenamide;
NCIt synonyms : L-Alanine, N-((S)-(((1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy)methyl)phenoxyphosphinyl)-,
1-Methylethyl Ester; TFV Alafenamide;
NCIt definition : A lipophilic phosphonamidate prodrug of tenofovir, a synthetic antiviral acyclic nucleotide
analog of adenosine 5-monophosphate and a nucleoside reverse transcriptase inhibitor
(NRTI), with antiviral activity against hepatitis B virus (HBV) and potentially against
human immunodeficiency virus (HIV). Upon oral administration, tenofovir alafenamide
is taken up by hepatocytes through passive diffusion and through the hepatic uptake
transporters organic anion transporting polypeptides 1B1 (OATP1B1) and 1B3 (OATP1B3).
Inside the hepatocytes, tenofovir alafenamide is hydrolyzed and converted to tenofovir
by carboxylesterase 1 (CES1). Intracellular tenofovir is phosphorylated by cellular
kinases to its pharmacologically active form, tenofovir diphosphate. Tenofovir diphosphate
is incorporated into viral DNA instead of the natural substrate deoxyadenosine 5-triphosphate,
and inhibits HBV reverse transcriptase, resulting in DNA chain-termination and inhibition
of HBV replication. In addition, tenofovir diphosphate is incorporated into HIV DNA
instead of the natural substrate deoxyadenosine 5-triphosphate, thereby inhibiting
HIV-1 reverse transcriptase (RT) and resulting in DNA chain termination and impairment
of HIV replication.;
UNII : EL9943AG5J;
InChIKey : LDEKQSIMHVQZJK-GNGHXOLXSA-N;
CAS number : 379270-37-8;
Molecule name : GS 7340; GS-7340;
NCI Metathesaurus CUI : CL550911;
Origin ID : C148276;
UMLS CUI : C3713958;
Automatic exact mappings (from CISMeF team)
- Currated CISMeF NLP mapping
- Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
