KEGG   DRUG: Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
Entry
D11382            Mixture   Drug                                   
Name
Darunavir, cobicistat, emtricitabine and tenofovir alafenamide;
Symtuza (TN)
Product
Component
(Darunavir [DR:D03656] | Darunavir ethanolate [DR:D06478]), Cobicistat [DR:D09881], Emtricitabine [DR:D01199], (Tenofovir alafenamide [DR:D10428] | Tenofovir alafenamide fumarate [DR:D10605])
Class
Antiviral
 DG03107  Anti-HIV agent
Metabolizing enzyme substrate
 DG01644  CYP2D6 substrate
 DG01633  CYP3A/CYP3A4 substrate
Metabolizing enzyme inhibitor
 DG01645  CYP2D6 inhibitor
 DG02852  CYP3A/CYP3A4 inhibitor
Transporter substrate
 DG01665  ABCB1 substrate
 DG03001  CTSA substrate
Transporter inhibitor
 DG01622  ABCB1 inhibitor
 DG02862  ABCG2 inhibitor
 DG02865  SLCO1B1 inhibitor
 DG02907  SLCO1B3 inhibitor
Remark
Therapeutic category: 6250
ATC code: J05AR22
Product: D11382<JP/US>
Efficacy
Antiviral
  Disease
HIV-1 infection [DS:H01563]
Comment
Darunavir is a substrate of CYP3A; it is also an inhibitor of CYP3A, CYP2D6 and P-gp.
Cobicistat is metabolized by CYP3A and CYP2D6 and inhibits CYP3A, CYP2D6, P-gp, BCRP, OATP1B1 and OATP1B3.
Tenofovir alafenamide is a substrate of CTSA, CYP3A and P-gp.
Target
HIV protease [KO:K22599]
HIV-1 reverse transcriptase [KO:K24802]
  Pathway
ko03230  Viral genome structure
ko03240  Viral replication
ko03250  Viral life cycle - HIV-1
Metabolism
Enzyme: CYP3A [HSA:1576 1577 1551], CYP2D6 [HSA:1565], CTSA [HSA:5476]
Transporter: ABCB1 [HSA:5243]
Interaction
CYP inhibition: CYP3A [HSA:1576 1577 1551], CYP2D6 [HSA:1565]
Transporter inhibition: ABCB1 [HSA:5243], ABCG2 [HSA:9429], SLCO1B1 [HSA:10599], SLCO1B3 [HSA:28234]
Brite
Anatomical Therapeutic Chemical (ATC) classification [BR:br08303]
 J ANTIINFECTIVES FOR SYSTEMIC USE
  J05 ANTIVIRALS FOR SYSTEMIC USE
   J05A DIRECT ACTING ANTIVIRALS
    J05AR Antivirals for treatment of HIV infections, combinations
     J05AR22 Emtricitabine, tenofovir alafenamide, darunavir and cobicistat
      D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide <JP/US>
USP drug classification [BR:br08302]
 Antivirals
  Anti-HIV Combinations
   Cobicistat/ Darunavir/ Emtricitabine/ Tenofovir Alafenamide
    D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
Therapeutic category of drugs in Japan [BR:br08301]
 6  Agents against pathologic organisms and parasites
  62  Chemotherapeutics
   625  Antivirals
    6250  Antivirals
     D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
Drug groups [BR:br08330]
 Antiviral
  DG03107  Anti-HIV agent
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
 Metabolizing enzyme substrate
  DG01644  CYP2D6 substrate
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
  DG01633  CYP3A/CYP3A4 substrate
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
 Metabolizing enzyme inhibitor
  DG01645  CYP2D6 inhibitor
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
  DG02852  CYP3A/CYP3A4 inhibitor
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
 Transporter substrate
  DG01665  ABCB1 substrate
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
  DG03001  CTSA substrate
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
 Transporter inhibitor
  DG01622  ABCB1 inhibitor
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
  DG02862  ABCG2 inhibitor
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
  DG02865  SLCO1B1 inhibitor
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
  DG02907  SLCO1B3 inhibitor
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
Drug classes [BR:br08332]
 Antiviral
  DG03107  Anti-HIV agent
   D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide
Antimicrobials [BR:br08307]
 Antivirals
  Polyprotein cleavage inhibitor
   HIV protease inhibitor
    D11382  Darunavir, cobicistat, emtricitabine and tenofovir alafenamide <JP/US>
New drug approvals in Europe [br08329.html]
 European public assessment reports (EPAR) authorised medicine
  D11382
Drug metabolizing enzymes and transporters [br08309.html]
 Drug metabolizing enzymes
  D11382
 Drug transporters
  D11382
Other DBs
PubChem: 384585360
LinkDB

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