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- NCIT_C173644 IAO_0000115 "A four-drug fixed combination of the ethanolate salt form of darunavir, a human immunodeficiency virus type 1 (HIV-1) protease nonpeptidic inhibitor; cobicistat, a cytochrome P450 3A (CYP3A) inhibitor; emtricitabine, a nucleoside reverse transcriptase (RT) inhibitor (NRTI) analog of cytidine; and tenofovir alafenamide fumarate, the fumarate salt form of the lipophilic phosphonamidate prodrug of tenofovir, a NRTI analog of adenosine monophosphate, that is used to treat human immunodeficiency virus (HIV) infection. Upon oral administration of darunavir ethanolate/cobicistat/emtricitabine/tenofovir alafenamide fumarate, darunavir selectively targets and binds to the active site of HIV-1 protease and inhibits the dimerization and catalytic activity of HIV-1 protease. This inhibits the proteolytic cleavage of viral Gag and Gag-Pol polyproteins in HIV-infected cells. This inhibition leads to the production of immature, non-infectious viral proteins that are unable to form mature virions, and prevents HIV replication. Cobicistat inhibits CYP3A, thereby limiting the oxidative metabolism of darunavir and increases its systemic exposure. Emtricitabine and tenofovir alafenamide, after being converted in vivo to tenofovir, inhibit the activity of HIV RT by competing with natural deoxyribonucleosides for incorporation into the growing viral DNA chain and resulting in early chain termination. This interferes with the generation of DNA copies of viral RNA, which is necessary for the synthesis of new virions." @default.
- NCIT_C173644 NCIT_NHC0 "C173644" @default.
- NCIT_C173644 NCIT_P106 "Pharmacologic Substance" @default.
- NCIT_C173644 NCIT_P108 "Darunavir Ethanolate/Cobicistat/Emtricitabine/Tenofovir Alafenamide Fumarate" @default.
- NCIT_C173644 NCIT_P208 "CL1407368" @default.
- NCIT_C173644 normalizedInformationContent "100" @default.
- NCIT_C173644 referenceCount "1" @default.
- NCIT_C173644 hasExactSynonym "Darunavir Ethanolate/Cobicistat/Emtricitabine/Tenofovir Alafenamide Fumarate" @default.
- NCIT_C173644 hasExactSynonym "Symtuza" @default.
- NCIT_C173644 type Class @default.
- NCIT_C173644 isDefinedBy ncit.owl @default.
- NCIT_C173644 label "Darunavir Ethanolate/Cobicistat/Emtricitabine/Tenofovir Alafenamide Fumarate" @default.
- NCIT_C173644 subClassOf NCIT_C1660 @default.
- NCIT_C173644 subClassOf NCIT_C173644 @default.
- NCIT_C173644 subClassOf NCIT_C1908 @default.
- NCIT_C173644 subClassOf NCIT_C1909 @default.
- NCIT_C173644 subClassOf NCIT_C254 @default.
- NCIT_C173644 subClassOf NCIT_C281 @default.