Tenofovir alafenamide (free base)
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Hodoodo CAT#: H314270

CAS#: 379270-37-8 (free base)

Description: Tenofovir alafenamide, also known as TAF and GS-7340, is a nucleotide reverse transcriptase inhibitor (NRTIs) and a novel prodrug of tenofovir. By blocking reverse transcriptase, TAF prevent HIV from multiplying and can reduce the amount of HIV in the body. Tenofovir alafenamide is a prodrug, which means that it is an inactive drug. In the body, tenofovir alafenamide is converted to tenofovir diphosphate (TFV-DP). Tenofovir alafenamide fumarate was approved in November 2015 for treatment of HIV-1.


Chemical Structure

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Tenofovir alafenamide (free base)
CAS# 379270-37-8 (free base)

Theoretical Analysis

Hodoodo Cat#: H314270
Name: Tenofovir alafenamide (free base)
CAS#: 379270-37-8 (free base)
Chemical Formula: C21H29N6O5P
Exact Mass: 476.19
Molecular Weight: 476.470
Elemental Analysis: C, 52.94; H, 6.13; N, 17.64; O, 16.79; P, 6.50

Price and Availability

Size Price Availability Quantity
100mg USD 150 Ready to ship
200mg USD 250 Ready to ship
500mg USD 450 Ready to ship
1g USD 750 Ready to ship
2g USD 1250 Ready to ship
5g USD 2650 Ready to ship
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Related CAS #: 379270-38-9 (fumarate)   1392275-56-7 (hemifumarate)   379270-37-8 (free base)  

Synonym: GS7340; GS-7340; GS 7340; TAF; Tenofovir alafenamide; Genvoya.

IUPAC/Chemical Name: (S)-isopropyl 2-(((S)-((((R)-1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)(phenoxy)phosphoryl)amino)propanoate

InChi Key: LDEKQSIMHVQZJK-AZFZMOAFSA-N

InChi Code: InChI=1S/C21H29N6O5P/c1-14(2)31-21(28)16(4)26-33(29,32-17-8-6-5-7-9-17)13-30-15(3)10-27-12-25-18-19(22)23-11-24-20(18)27/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24)/t15-,16+,33?/m1/s1

SMILES Code: C[C@H](N[P@@](OC1=CC=CC=C1)(CO[C@H](C)CN2C=NC3=C(N)N=CN=C23)=O)C(OC(C)C)=O

Appearance: White to off-white solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO.

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: Related CAS# CAS#379270-38-9 =Tenofovir alafenamide fumarate, 1:1 CAS#1392275-56-7= Tenofovir alafenamide hemifumarate, 2:1 CAS#379270-37-8 = Tenofovir alafenamide

Biological target:
In vitro activity:
In vivo activity:

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 73.0 153.21
Water 3.3 7.01
Ethanol 55.0 115.43
DMF 25.0 52.47
PBS (pH 7.2) 2.0 4.20

Preparing Stock Solutions

The following data is based on the product molecular weight 476.47 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Shafran SD, Di Perri G, Esser S, Lelièvre JD, Parczewski M. Planning HIV therapy to prevent future comorbidities: patient years for tenofovir alafenamide. HIV Med. 2019 Jun;20 Suppl 7:1-16. doi: 10.1111/hiv.12755. Review. PubMed PMID: 31099116.

2: Bictegravir/emtricitabine/tenofovir alafenamide for HIV infection. Aust Prescr. 2019 Apr;42(2):68-69. doi: 10.18773/austprescr.2019.016. Epub 2019 Feb 28. Review. PubMed PMID: 31048941; PubMed Central PMCID: PMC6478953.

3: Common Drug Review New Combination Product Submission: Darunavir/Cobicistat/Emtricitabine/Tenofovir alafenamide (Symtuza): (Janssen Canada Inc.): Indication: A complete regimen for the treatment of HIV type 1 infection in adults and adolescents (aged 12 years and older with body weight at least 40 kg) with no known mutations associated with resistance to the individual components of Symtuza [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Aug. Available from http://www.ncbi.nlm.nih.gov/books/NBK540525/ PubMed PMID: 31034191.

4: CADTH Canadian Drug Expert Committee Recommendation: Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide (Symtuza — Janssen Inc.): Indication: Treatment of HIV type 1 (HIV-1) infection [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Jul. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK540287/ PubMed PMID: 31013021.

5: Clinical Review Report: Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/FTC/TAF) (Biktarvy): (Gilead Sciences Canada, Inc.): Indication: A complete regimen for the treatment of HIV-1 infection in adults with no known substitution associated with resistance to the individual components of Biktarvy [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Oct. Available from http://www.ncbi.nlm.nih.gov/books/NBK539526/ PubMed PMID: 30958669.

6: Pharmacoeconomic Review Report: Bictegravir/Emtricitabine/Tenofovir Alafenamide (B/FTC/TAF) (Biktarvy): (Gilead Sciences Canada, Inc.): Indication: A complete regimen for the treatment of HIV-1 infection in adults with no known substitution associated with resistance the individual components of Biktarvy [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Oct. Available from http://www.ncbi.nlm.nih.gov/books/NBK539546/ PubMed PMID: 30958667.

7: CADTH Canadian Drug Expert Committee Recommendation: Bictegravir/Emtricitabine/Tenofovir Alafenamide (Biktarvy — Gilead Sciences Canada, Inc.): Indication: As a complete regimen for the treatment of human immunodeficiency virus-1 (HIV-1) infection in adults with no known substitution associated with resistance to the individual components of Biktarvy [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Oct. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK539326/ PubMed PMID: 30942994.

8: Pharmacoeconomic Review Report: Emtricitabine/tenofovir alafenamide (Descovy) [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2016 Aug. Available from http://www.ncbi.nlm.nih.gov/books/NBK539225/ PubMed PMID: 30933443.

9: Clinical Review Report: Emtricitabine/tenofovir alafenamide fumarate (Descovy) [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2016 Aug. Available from http://www.ncbi.nlm.nih.gov/books/NBK538758/ PubMed PMID: 30883070.

10: CADTH Canadian Drug Expert Committee Final Recommendation: Emtricitabine/Tenofovir Alafenamide: (Descovy — Gilead Sciences Canada, Inc.): Indication: HIV-1 Infection [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2016 Aug. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK538372/ PubMed PMID: 30860687.

11: Pham HT, Mesplède T. Bictegravir in a fixed-dose tablet with emtricitabine and tenofovir alafenamide for the treatment of HIV infection: pharmacology and clinical implications. Expert Opin Pharmacother. 2019 Mar;20(4):385-397. doi: 10.1080/14656566.2018.1560423. Epub 2019 Jan 30. Review. PubMed PMID: 30698467.

12: Giacomet V, Cossu MV, Capetti AF, Zuccotti G, Rizzardini G. An evaluation of elvitegravir plus cobicistat plus tenofovir alafenamide plus emtricitabine as a single-tablet regimen for the treatment of HIV in children and adolescents. Expert Opin Pharmacother. 2019 Feb;20(3):269-276. doi: 10.1080/14656566.2018.1559299. Epub 2018 Dec 26. Review. PubMed PMID: 30586314.

13: Clinical Review Report: Tenofovir Alafenamide (Vemlidy): (Gilead Sciences Canada, Inc.): Indication: Treatment of chronic hepatitis B in adults with compensated liver disease [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Apr. Available from http://www.ncbi.nlm.nih.gov/books/NBK533926/ PubMed PMID: 30475544.

14: Hill L, Smith SR, Karris MY. Profile of bictegravir/emtricitabine/tenofovir alafenamide fixed dose combination and its potential in the treatment of HIV-1 infection: evidence to date. HIV AIDS (Auckl). 2018 Oct 29;10:203-213. doi: 10.2147/HIV.S145529. eCollection 2018. Review. PubMed PMID: 30464641; PubMed Central PMCID: PMC6214311.

15: Squillace N, Bozzi G, Colella E, Gori A, Bandera A. Darunavir-cobicistat-emtricitabine-tenofovir alafenamide: safety and efficacy of a protease inhibitor in the modern era. Drug Des Devel Ther. 2018 Oct 29;12:3635-3643. doi: 10.2147/DDDT.S147493. eCollection 2018. Review. PubMed PMID: 30464395; PubMed Central PMCID: PMC6211373.

16: 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. Review. Erratum in: Drugs. 2019 Mar 22;:. PubMed PMID: 30460547; PubMed Central PMCID: PMC6424950.

17: Pharmacoeconomic Review Report: Tenofovir Alafenamide (Vemlidy): (Gilead Sciences Canada, Inc.): Indication: Treatment of chronic hepatitis B in adults with compensated liver disease [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Apr. Available from http://www.ncbi.nlm.nih.gov/books/NBK532825/ PubMed PMID: 30427623.

18: CADTH Canadian Drug Expert Committee Recommendation: Tenofovir Alafenamide (Vemlidy - Gilead Sciences Canada, Inc.): Indication: Chronic Hepatitis B [Internet]. Ottawa (ON): Canadian Agency for Drugs and Technologies in Health; 2018 Mar 28. No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK532703/ PubMed PMID: 30403460.

19: Childs-Kean LM, Egelund EF, Jourjy J. Tenofovir Alafenamide for the Treatment of Chronic Hepatitis B Monoinfection. Pharmacotherapy. 2018 Oct;38(10):1051-1057. doi: 10.1002/phar.2174. Epub 2018 Sep 9. Review. PubMed PMID: 30120841.

20: Byrne R, Carey I, Agarwal K. Tenofovir alafenamide in the treatment of chronic hepatitis B virus infection: rationale and clinical trial evidence. Therap Adv Gastroenterol. 2018 Jul 16;11:1756284818786108. doi: 10.1177/1756284818786108. eCollection 2018. Review. PubMed PMID: 30034532; PubMed Central PMCID: PMC6048601.