Peringatan Keamanan

The LD50 of tenofovir alafenamide has not been reported. In cases of overdose, continuous monitoring of vital signs is required as the adverse effects in high doses has not been evaluated. However, in case of overdose, tenofovir is efficiently removed by hemodialysis with an extraction coefficient of 54%.L6286

Carcinogenic reports have only been performed with tenofovir disoproxil and it is important to consider that tenofovir alafenamide does not present a high systemic exposure. However, long-term exposure with 10-fold dosages of tenofovir disoproxil was reported to produce liver adenomas in females. Tenofovir alafenamide was not reported to present mutagenic potential and it did not present effects on fertility.L6286

Tenofovir alafenamide

DB09299

small molecule approved

Deskripsi

Tenofovir alafenamide is a novel tenofovir prodrug developed in order to improve renal safety when compared to the counterpart tenofovir disoproxil.A178060 Both of these prodrugs were first created to cover the polar phosphonic acid group on tenofovir by using a novel oxycarbonyloxymethyl linkers to improve the oral bioavailability and intestinal diffusion.T239 Tenofovir alafenamide is an alanine ester form characterized for presenting low systemic levels but high intracellular concentration.A178219 It has been reported to produce a large antiviral efficacy at doses ten times lower than tenofovir disoproxil.A178327 Tenofovir alafenamide is indicated to treat chronic hepatitis B,L6241 treat HIV-1,L4388,L6277,L6280,L6283 and prevent HIV-1 infections.L4388,L9010

Tenofovir alafenamide was developed by Gilead Sciences Inc and granted FDA approval on 5 November 2015.L6271

Struktur Molekul 2D

Berat 476.474
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The reported half-life for tenofovir alafenamide is of 0.51 hours.[A178231]
Volume Distribusi In clinical trials, the reported volume of distribution of tenofovir alafenamide was higher than 100 L.[A178438]
Klirens (Clearance) The reported clearance rate of tenofovir alafenamide is 117 L/h. In patients with severe renal impairment, this value can be decreased by 50%, reporting a rate of 61.7 L/h.[L6337]

Absorpsi

As compared to the parent molecule, tenofovir, tenofovir alafenamide presents a lipophilic group that masks the negative charge of the parent moiety which improves its oral bioavailability.A178060 Tenofovir alafenamide is highly stable in plasma and, after administration of this prodrug, there is a low concentration of tenofovir in plasma. After oral administration, tenofovir alafenamide is rapidly absorbed by the gut. When a single dose is administered, a peak concentration of 16 ng/ml of the parent compound, corresponding to about 73% of the dose, is observed after 2 hours with an AUC of 270 ng\*h/mL.A178060, A18473 Once inside the body, tenofovir alafenamide enters hepatocytes by passive diffusion regulated by the organic anion transporters 1B1 and 1B3 for its activation.A178249 Administration of tenofovir alafenamide concomitantly with a high-fat meal results in an increase of about 65% in its internal exposure.L6286

Metabolisme

To be activated, tenofovir alafenamide is required to be hydrolyzed to the parent compound tenofovir by the activity of cathepsin A or carboxylesterase 1. Tenofovir alafenamide presents significant plasma stability and hence, its activation is performed inside the target cells.A178060 After activation, tenofovir is further processed and after 1-2 days, it is detected in plasma almost completely transformed to uric acid.A178060

Rute Eliminasi

Tenofovir alafenamide has been registered to present a bile elimination that corresponds to 47% of the administered dose and a renal elimination the represents about 36%. From the recovered dose in urine, about 75% is represented as unchanged tenofovir followed by uric acid and a small dose of tenofovir alafenamide. On the other hand, in feces, 99% of the recovered dose corresponds to tenofovir.A178060

Interaksi Makanan

3 Data
  • 1. Avoid St. John's Wort. St. John's Wort can cause drug interaction and decrease the serum concentration of tenofovir alafenamide.
  • 2. Take at the same time every day.
  • 3. Take with or without food. Recommendations vary from product to product - consult individual product monographs for additional information.

Interaksi Obat

1318 Data
Phenytoin The serum concentration of Tenofovir alafenamide can be decreased when it is combined with Phenytoin.
Fosphenytoin The serum concentration of Tenofovir alafenamide can be decreased when it is combined with Fosphenytoin.
Atazanavir The serum concentration of Atazanavir can be decreased when it is combined with Tenofovir alafenamide.
Didanosine The serum concentration of Didanosine can be increased when it is combined with Tenofovir alafenamide.
Simeprevir The serum concentration of Tenofovir alafenamide can be increased when it is combined with Simeprevir.
Telaprevir The serum concentration of Tenofovir alafenamide can be increased when it is combined with Telaprevir.
Tipranavir The serum concentration of Tenofovir alafenamide can be decreased when it is combined with Tipranavir.
Taxifolin Taxifolin may decrease the excretion rate of Tenofovir alafenamide which could result in a higher serum level.
Licofelone Licofelone may decrease the excretion rate of Tenofovir alafenamide which could result in a higher serum level.
Polmacoxib Polmacoxib may decrease the excretion rate of Tenofovir alafenamide which could result in a higher serum level.
Ebselen Ebselen may decrease the excretion rate of Tenofovir alafenamide which could result in a higher serum level.
Flurbiprofen axetil Flurbiprofen axetil may decrease the excretion rate of Tenofovir alafenamide which could result in a higher serum level.
Foscarnet The risk or severity of nephrotoxicity can be increased when Tenofovir alafenamide is combined with Foscarnet.
Mannitol The serum concentration of Tenofovir alafenamide can be increased when it is combined with Mannitol.
Icosapent Icosapent may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefotiam Cefotiam may increase the nephrotoxic activities of Tenofovir alafenamide.
Mesalazine The risk or severity of nephrotoxicity can be increased when Mesalazine is combined with Tenofovir alafenamide.
Cefmenoxime Cefmenoxime may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefmetazole Cefmetazole may increase the nephrotoxic activities of Tenofovir alafenamide.
Pamidronic acid Pamidronic acid may increase the nephrotoxic activities of Tenofovir alafenamide.
Tenofovir disoproxil The serum concentration of Tenofovir alafenamide can be increased when it is combined with Tenofovir disoproxil.
Indomethacin Indomethacin may increase the nephrotoxic activities of Tenofovir alafenamide.
Cidofovir The serum concentration of Tenofovir alafenamide can be increased when it is combined with Cidofovir.
Triamterene Triamterene may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefpiramide Cefpiramide may increase the nephrotoxic activities of Tenofovir alafenamide.
Ceftazidime The serum concentration of Tenofovir alafenamide can be increased when it is combined with Ceftazidime.
Loracarbef Loracarbef may increase the nephrotoxic activities of Tenofovir alafenamide.
Framycetin Framycetin may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefalotin Cefalotin may increase the nephrotoxic activities of Tenofovir alafenamide.
Nabumetone Nabumetone may increase the nephrotoxic activities of Tenofovir alafenamide.
Ketorolac Ketorolac may increase the nephrotoxic activities of Tenofovir alafenamide.
Tenoxicam Tenoxicam may increase the nephrotoxic activities of Tenofovir alafenamide.
Amikacin Amikacin may increase the nephrotoxic activities of Tenofovir alafenamide.
Celecoxib Celecoxib may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefotaxime Cefotaxime may increase the nephrotoxic activities of Tenofovir alafenamide.
Tolmetin Tolmetin may increase the nephrotoxic activities of Tenofovir alafenamide.
Rofecoxib Rofecoxib may increase the nephrotoxic activities of Tenofovir alafenamide.
Piroxicam The serum concentration of Tenofovir alafenamide can be increased when it is combined with Piroxicam.
Methotrexate The serum concentration of Tenofovir alafenamide can be increased when it is combined with Methotrexate.
Cephalexin The serum concentration of Tenofovir alafenamide can be increased when it is combined with Cephalexin.
Fenoprofen Fenoprofen may increase the nephrotoxic activities of Tenofovir alafenamide.
Valaciclovir The serum concentration of Tenofovir alafenamide can be increased when it is combined with Valaciclovir.
Valdecoxib Valdecoxib may increase the nephrotoxic activities of Tenofovir alafenamide.
Diclofenac Diclofenac may increase the nephrotoxic activities of Tenofovir alafenamide.
Sulindac Sulindac may increase the nephrotoxic activities of Tenofovir alafenamide.
Bacitracin Bacitracin may increase the nephrotoxic activities of Tenofovir alafenamide.
Amphotericin B Amphotericin B may increase the nephrotoxic activities of Tenofovir alafenamide.
Tobramycin The serum concentration of Tenofovir alafenamide can be increased when it is combined with Tobramycin.
Cephaloglycin Cephaloglycin may increase the nephrotoxic activities of Tenofovir alafenamide.
Furosemide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Furosemide.
Flurbiprofen The serum concentration of Tenofovir alafenamide can be increased when it is combined with Flurbiprofen.
Pentamidine Pentamidine may increase the nephrotoxic activities of Tenofovir alafenamide.
Etodolac The serum concentration of Tenofovir alafenamide can be increased when it is combined with Etodolac.
Mefenamic acid Mefenamic acid may increase the nephrotoxic activities of Tenofovir alafenamide.
Acyclovir The serum concentration of Tenofovir alafenamide can be increased when it is combined with Acyclovir.
Naproxen Naproxen may increase the nephrotoxic activities of Tenofovir alafenamide.
Sulfasalazine The serum concentration of Tenofovir alafenamide can be increased when it is combined with Sulfasalazine.
Gentamicin Gentamicin may increase the nephrotoxic activities of Tenofovir alafenamide.
Phenylbutazone Phenylbutazone may increase the nephrotoxic activities of Tenofovir alafenamide.
Meloxicam Meloxicam may increase the nephrotoxic activities of Tenofovir alafenamide.
Carprofen Carprofen may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefaclor The serum concentration of Tenofovir alafenamide can be increased when it is combined with Cefaclor.
Diflunisal The serum concentration of Tenofovir alafenamide can be increased when it is combined with Diflunisal.
Bumetanide The serum concentration of Tenofovir alafenamide can be increased when it is combined with Bumetanide.
Etacrynic acid Etacrynic acid may increase the nephrotoxic activities of Tenofovir alafenamide.
Ceforanide Ceforanide may increase the nephrotoxic activities of Tenofovir alafenamide.
Salicylic acid Salicylic acid may increase the nephrotoxic activities of Tenofovir alafenamide.
Meclofenamic acid The serum concentration of Tenofovir alafenamide can be increased when it is combined with Meclofenamic acid.
Acetylsalicylic acid The serum concentration of Tenofovir alafenamide can be increased when it is combined with Acetylsalicylic acid.
Netilmicin Netilmicin may increase the nephrotoxic activities of Tenofovir alafenamide.
Carboplatin The serum concentration of Tenofovir alafenamide can be increased when it is combined with Carboplatin.
Oxaprozin The serum concentration of Tenofovir alafenamide can be increased when it is combined with Oxaprozin.
Hydrochlorothiazide Hydrochlorothiazide may increase the nephrotoxic activities of Tenofovir alafenamide.
Ketoprofen The serum concentration of Tenofovir alafenamide can be increased when it is combined with Ketoprofen.
Balsalazide Balsalazide may increase the nephrotoxic activities of Tenofovir alafenamide.
Ibuprofen The serum concentration of Tenofovir alafenamide can be increased when it is combined with Ibuprofen.
Cefditoren Cefditoren may increase the nephrotoxic activities of Tenofovir alafenamide.
Streptomycin The serum concentration of Tenofovir alafenamide can be increased when it is combined with Streptomycin.
Colistimethate Colistimethate may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefuroxime Cefuroxime may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefapirin Cefapirin may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefadroxil The serum concentration of Tenofovir alafenamide can be increased when it is combined with Cefadroxil.
Cefprozil Cefprozil may increase the nephrotoxic activities of Tenofovir alafenamide.
Kanamycin Kanamycin may increase the nephrotoxic activities of Tenofovir alafenamide.
Ceftriaxone The serum concentration of Tenofovir alafenamide can be increased when it is combined with Ceftriaxone.
Olsalazine The risk or severity of nephrotoxicity can be increased when Tenofovir alafenamide is combined with Olsalazine.
Lumiracoxib Lumiracoxib may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefamandole Cefamandole may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefazolin Cefazolin may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefonicid Cefonicid may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefoperazone Cefoperazone may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefotetan The serum concentration of Tenofovir alafenamide can be increased when it is combined with Cefotetan.
Cefoxitin Cefoxitin may increase the nephrotoxic activities of Tenofovir alafenamide.
Ceftizoxime Ceftizoxime may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefradine The serum concentration of Tenofovir alafenamide can be increased when it is combined with Cefradine.
Magnesium salicylate Magnesium salicylate may increase the nephrotoxic activities of Tenofovir alafenamide.
Salsalate Salsalate may increase the nephrotoxic activities of Tenofovir alafenamide.
Choline magnesium trisalicylate Choline magnesium trisalicylate may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefepime Cefepime may increase the nephrotoxic activities of Tenofovir alafenamide.
Cefacetrile Cefacetrile may increase the nephrotoxic activities of Tenofovir alafenamide.

Target Protein

Reverse transcriptase/RNaseH pol
Gag-Pol polyprotein gag-pol
Reverse transcriptase rt
DNA polymerase

Referensi & Sumber

Artikel (PubMed)
  • PMID: 27438578
    Aloy B, Tazi I, Bagnis CI, Gauthier M, Janus N, Launay-Vacher V, Deray G, Tourret J: Is Tenofovir Alafenamide Safer than Tenofovir Disoproxil Fumarate for the Kidneys? AIDS Rev. 2016 Oct-Dec;18(4):184-192.
  • PMID: 26859637
    Grant PM, Cotter AG: Tenofovir and bone health. Curr Opin HIV AIDS. 2016 May;11(3):326-32. doi: 10.1097/COH.0000000000000248.
  • PMID: 30460547
    Deeks ED: Bictegravir/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection. Drugs. 2018 Nov;78(17):1817-1828. doi: 10.1007/s40265-018-1010-7.
  • PMID: 29158666
    Ogawa E, Furusyo N, Nguyen MH: Tenofovir alafenamide in the treatment of chronic hepatitis B: design, development, and place in therapy. Drug Des Devel Ther. 2017 Nov 6;11:3197-3204. doi: 10.2147/DDDT.S126742. eCollection 2017.
  • PMID: 26640223
    Ray AS, Fordyce MW, Hitchcock MJ: Tenofovir alafenamide: A novel prodrug of tenofovir for the treatment of Human Immunodeficiency Virus. Antiviral Res. 2016 Jan;125:63-70. doi: 10.1016/j.antiviral.2015.11.009. Epub 2015 Nov 27.
  • PMID: 26952360
    Antela A, Aguiar C, Compston J, Hendry BM, Boffito M, Mallon P, Pourcher-Martinez V, Di Perri G: The role of tenofovir alafenamide in future HIV management. HIV Med. 2016 May;17 Suppl 2:4-16. doi: 10.1111/hiv.12401.
  • PMID: 24508897
    Markowitz M, Zolopa A, Squires K, Ruane P, Coakley D, Kearney B, Zhong L, Wulfsohn M, Miller MD, Lee WA: Phase I/II study of the pharmacokinetics, safety and antiretroviral activity of tenofovir alafenamide, a new prodrug of the HIV reverse transcriptase inhibitor tenofovir, in HIV-infected adults. J Antimicrob Chemother. 2014 May;69(5):1362-9. doi: 10.1093/jac/dkt532. Epub 2014 Feb 6.
Textbook
  • Taylor JB, Triggle DJ. (2007). Comprehensive Medicinal Chemistry II. Elsevier.

Contoh Produk & Brand

Produk: 45 • International brands: 0
Produk
  • Biktarvy
    Tablet • - • Oral • US • Approved
  • Biktarvy
    Tablet • - • Oral • US • Approved
  • Biktarvy
    Tablet • - • Oral • US • Approved
  • Biktarvy
    Tablet • - • Oral • Canada • Approved
  • Biktarvy
    Tablet • - • Oral • US • Approved
  • Biktarvy
    Tablet • - • Oral • US • Approved
  • Biktarvy
    Tablet, film coated • - • Oral • EU • Approved
  • Biktarvy
    Tablet, film coated • - • Oral • EU • Approved
Menampilkan 8 dari 45 produk.

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul