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[CAS NO. 1392275-56-7] Tenofoviralafenamidehemifumarate

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Catalog:	HY-15232B
Brand:	MCE
CAS:	1392275-56-7

Overview

MDL	MFCD30534429
Molecular Weight	534.50
Molecular Formula	C21H29N6O5P.1/2C4H4O4
SMILES	O=C(O)/C=C/C(O)=O.NC1=NC=NC2=C1N=CN2C[C@@H](C)OC[P@](OC3=CC=CC=C3)(N[C@@H](C)C(OC(C)C)=O)=O.[0.5]

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

[1]J Gastroenterol. 2020 Apr;55(4):441-452
[2]J Antimicrob Chemother. 2017 Jun 1;72(6):1731-1740.
[3]Antimicrob Agents Chemother. 2019 Mar 27;63(4). pii: e02143-18.
[4]Pharmaceutics. 2021, 13(10), 1656.

Summary

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an investigational oral prodrug of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor .

IC50 & Target

HIV-1

HIV-2

In Vitro

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC ₅₀ varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC ₅₀ s range from 0.1 to 12 nM, with a mean EC ₅₀ of 3.5 nM compared to a mean EC ₅₀ of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC ₅₀ s are 1.8 nM for TAF and 6.4 nM for AZT ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Tenofovir alafenamide hemifumarate (GS-7340 hemifumarate) is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF) ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04129554	Janssen Sciences Ireland UC	Hepatitis B, Chronic	November 6, 2019	Phase 2
NCT04850950	The First Affiliated Hospital of Zhengzhou University\|National Natural Science Foundation of China\|Henan Provincial People´s Hospital\|The Sixth People´s Hospital of Zhengzhou\|The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School\|Second Affiliated Hospital of Xi´an Jiaotong University\|Shandong Provincial Hospital\|Luoyang Central Hospital\|First Affiliated Hospital of Nanyang Medical College\|Sixth People´s Hospital of Kaifeng\|Luohe Central Hospital\|Xinyang Central Hospital\|Yan´an University Affiliated Hospital\|Nanyang Central Hospital\|Fifth People´s Hospital of Anyang	Chronic Hepatitis B\|Mother-to-Child Transmission\|Safety\|Efficacy\|Hepatitis B Virus\|Tenofovir Alafenamide Fumarate	April 26, 2021	Phase 4
NCT05001672	Taipei Veterans General Hospital, Taiwan	HBV\|Inflammatory Arthritis	August 15, 2021	Phase 4
NCT02904369	CONRAD\|United States Agency for International Development (USAID)\|Agility Clinical, Inc.	HIV	October 6, 2016	Phase 1
NCT04703465	RenJi Hospital	HBV\|Liver Transplant Disorder	April 1, 2021	Not Applicable
NCT04891770	Gilead Sciences\|Vir Biotechnology, Inc.	Chronic Hepatitis B	August 14, 2021	Phase 2
NCT04939441	Jidong Jia\|Beijing Ditan Hospital\|ShuGuang Hospital\|Tianjin Third Central Hospital\|Huashan Hospital\|The Sixth Peoples Hospital of Zhengzhou\|Tianjin Second People´s Hospital\|Ruijin Hospital\|Shanghai East Hospital\|Beijing Friendship Hospital	Chronic Hepatitis B	April 20, 2021	Phase 4
NCT04535544	Janssen Research & Development, LLC	Hepatitis D, Chronic	September 17, 2020	Phase 2
NCT04629976	Nucorion Pharmaceuticals, Inc.\|Ligand Pharmaceuticals	Chronic Hepatitis B	January 12, 2021	Phase 1
NCT03798119	Kaohsiung Medical University Chung-Ho Memorial Hospital	Hepatitis B\|Fibrosis and Cirrhosis of Liver	February 25, 2019	Phase 4
NCT03122262	Professor Francois Venter\|University of Witwatersrand, South Africa	HIV-1 Infection	January 16, 2017	Phase 3
NCT03471624	Stanford University\|Gilead Sciences	Hepatitis B, Chronic	May 1, 2018	Phase 4
NCT04439539	Janssen Research & Development, LLC	Hepatitis B, Chronic	September 14, 2020	Phase 2
NCT03695029	National Taiwan University Hospital	Hepatitis B Virus Infection	December 29, 2010	Phase 4
NCT04864366	Huashan Hospital	Chronic Hepatitis B	April 30, 2021
NCT02957864	Erasmus Medical Center\|Gilead Sciences	Renal Insufficiency,Chronic\|Hiv\|Therapeutic Agent Toxicity	October 2016	Phase 4
NCT04231565	Third Affiliated Hospital, Sun Yat-Sen University	Hepatitis B Virus	January 31, 2021	Not Applicable
NCT02357602	University of North Carolina, Chapel Hill\|Gilead Sciences	Healthy	March 2015	Phase 1
NCT05177926	Nanfang Hospital of Southern Medical University\|Gilead Sciences\|Tigermed Consulting Co., Ltd	Hepatitis B, Chronic\|Mother to Child Transmission	April 4, 2021	Phase 4
NCT04201808	New Discovery LLC\|Beijing Ditan Hospital	Hepatitis B, Chronic	May 1, 2021	Phase 4
NCT03753074	Young-Suk Lim\|Samsung Medical Center\|Kyunghee University Medical Center\|Chung-Ang University Hosptial, Chung-Ang University College of Medicine\|Seoul National University Hospital\|Ulsan University Hospital\|Konkuk University Medical Center\|Kyungpook National University Hospital\|Korea University Guro Hospital\|Seoul St. Mary´s Hospital\|Kaohsiung Medical University\|Chang Gung Memorial Hospital\|E-DA Hospital\|Taitung Mackay Memorial Hospital\|National Cheng-Kung University Hospital\|Chi Mei Medical Hospital\|Chiayi Christian Hospital\|St. Martin De Porress Hospital\|Dalin Tzu Chi General Hospital\|Taichung Veterans General Hospital\|China Medical University Hospital\|Asan Medical Center	Chronic Hepatitis b	February 18, 2019	Phase 4
NCT04195074	Third Affiliated Hospital, Sun Yat-Sen University	Chronic Hepatitis b	January 1, 2019	Not Applicable
NCT04059198	F-star Therapeutics, Inc.\|PRA Health Sciences	Hepatitis B\|HBV\|Hepatitis B, Chronic	October 10, 2019	Phase 2
NCT04211805	New Discovery LLC	Hepatitis B, Chronic\|Pregnancy Related	January 27, 2020
NCT05410496	Taichung Veterans General Hospital	Safety Issues	June 22, 2021	Phase 4
NCT02957994	Asian Pacific Liver Center at Coalition of Inclusive Medicine	Hepatitis B	December 22, 2016	Phase 4
NCT04674423	National Cheng-Kung University Hospital	Chronic Hepatitis b	May 14, 2020	Phase 4
NCT04616963	University of California, San Diego	Hiv\|Hormone Therapy	October 24, 2019	Phase 4
NCT04667104	Janssen Research & Development, LLC	Hepatitis B, Chronic	February 1, 2021	Phase 2
NCT00036634	Gilead Sciences	HIV Infections	March 2002	Phase 1\|Phase 2
NCT05244057	Shanghai HEP Pharmaceutical Co., Ltd.\|Shanghai Tong Ren Hospital\|Shanghai East Hospital	Chronic Hepatitis B	February 2022	Phase 2
NCT05195450	Institute of Liver and Biliary Sciences, India	Non-cirrhotic, Chronic Hepatitis B	February 23, 2022	Not Applicable
NCT05423106	Janssen Research & Development, LLC	Healthy\|Hepatitis B, Chronic	July 4, 2022	Phase 1
NCT03604016	IlDong Pharmaceutical Co Ltd	Hepatitis B	September 23, 2018	Phase 4
NCT04937881	University of California, Los Angeles\|University of Cape Town\|Desmond Tutu HIV Foundation\|Gilead Sciences	Hiv	June 13, 2022	Phase 3
NCT04070079	University Health Network, Toronto	Hepatitis B, Chronic	January 29, 2019	Phase 4
NCT01671787	Gilead Sciences	Chronic Hepatitis B	March 2012	Phase 1
NCT03887702	Southwest Oncology Group\|National Cancer Institute (NCI)	Hepatitis B Infection\|Malignant Solid Neoplasm	February 21, 2019	Phase 3
NCT04585737	Charlotte-Paige Rolle, MD\|ViiV Healthcare\|Orlando Immunology Center	HIV I Infection	September 22, 2020	Phase 4
NCT05467553	National Taiwan University Hospital\|PharmaEssentia	Hepatitis D	August 31, 2022	Phase 2
NCT05423834	Chinese University of Hong Kong	Chronic Hepatitis B	August 1, 2022
NCT05063071	Fudan University	HBV\|POST LIVER TRANSPLANT	July 29, 2021	Phase 4
NCT04391608	Mahidol University	Renal Insufficiency\|Tenofovir	November 9, 2019	Phase 4
NCT04518228	National Institute of Allergy and Infectious Diseases (NIAID)\|International Maternal Pediatric Adolescent AIDS Clinical Trials Group\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)\|National Institute of Mental Health (NIMH)\|Gilead Sciences\|ViiV Healthcare\|Merck Sharp & Dohme LLC	HIV Infections\|Tuberculosis	June 8, 2021
NCT03241641	Young-Suk Lim\|Samsung Medical Center\|Korea University Guro Hospital\|Konkuk University Medical Center\|Seoul National University Hospital\|Asan Medical Center	Chronic Hepatitis b	October 26, 2017	Phase 4
NCT04196998	Third Affiliated Hospital, Sun Yat-Sen University	Hepatitis B\|Compensated Cirrhosis	January 1, 2019	Not Applicable
NCT03804372	Gruppo Italiano Malattie EMatologiche dell´Adulto	Large-B-cell Diffuse Lymphoma\|Chronic Lymphoid Leukemia	July 7, 2020	Phase 2
NCT03646370	Thomas Jefferson University	HIV-1-infection\|Metabolic Syndrome\|Cardiovascular Diseases\|Weight Gain\|Renal Function Abnormal\|Hyperglycemia	July 25, 2018
NCT03115736	University Hospital Inselspital, Berne	HIV and Hepatitis B Coinfection	May 23, 2017	Phase 2
NCT04054089	Cristina Mussini\|University of Modena and Reggio Emilia	HIV Infections	September 2019	Phase 4
NCT04683341	Kaohsiung Medical University Chung-Ho Memorial Hospital	HBV	September 1, 2020	Phase 4
NCT04507607	Third Affiliated Hospital, Sun Yat-Sen University	Chronic Hepatitis B\|Mother-to-child Block\|Antiviral Treatment	August 1, 2020	Early Phase 1
NCT03489239	Thomas Jefferson University\|Gilead Sciences	Hepatitis B	November 16, 2017	Phase 3
NCT05583006	Taichung Veterans General Hospital	Patient Satisfaction\|Drug Adherence\|Efficacy, Self\|Safety Issues	December 1, 2022
NCT00042289	National Institute of Allergy and Infectious Diseases (NIAID)\|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)	HIV Infections	June 9, 2003
NCT03566030	Yonsei University	Hepatitis B\|Antiviral Drug Adverse Reaction	September 1, 2018
NCT03356834	Humanity and Health Research Centre	Chronic Hepatitis B	December 1, 2017	Phase 4
NCT03933384	Taichung Veterans General Hospital	Hepatitis B\|Viral Hepatitis	August 19, 2019	Phase 4
NCT04483674	Anna Cruceta\|Fundacion Clinic per a la Recerca Biomédica	HIV Primary Infection	December 4, 2020	Phase 2
NCT04619082	Chiayi Christian Hospital\|St. Martin De Porress Hospital\|Dalin Tzu Chi General Hospital\|National Taiwan University Hospital, Yun-Lin Branch\|Chi Mei Medical Hospital	Hepatitis B Reactivation	July 1, 2021	Phase 4
NCT05275023	Janssen Research & Development, LLC	Hepatitis B, Chronic	June 30, 2022	Phase 2
NCT04501224	Third Affiliated Hospital, Sun Yat-Sen University	Chronic Hepatitis b\|Cirrhosis Due to Hepatitis B	August 3, 2020	Not Applicable
NCT04585789	Janssen Research & Development, LLC	Hepatitis B	March 11, 2021	Phase 2
NCT03752658	Tongji Hospital\|Gilead Sciences	Chronic Hepatitis b	January 25, 2019
NCT02984852	Janssen Scientific Affairs, LLC	Healthy	December 2016	Phase 1
NCT03549689	Philip Grant\|Stanford University	HIV+AIDS\|HIV-1-infection\|Osteopenia	August 1, 2019	Phase 2
NCT05404919	University of Pennsylvania	Lung Transplant\|Hepatitis B	September 6, 2022	Phase 2
NCT02437110	National Institute of Neurological Disorders and Stroke (NINDS)\|National Institutes of Health Clinical Center (CC)	Amyotrophic Lateral Sclerosis	April 1, 2019	Phase 1
NCT05453448	Xiangya Hospital of Central South University	Antiviral Drugs	May 1, 2022	Not Applicable
NCT03920618	Third Affiliated Hospital, Sun Yat-Sen University	Hepatitis B\|Acute-On-Chronic Liver Failure	February 1, 2019	Not Applicable
NCT02995252	University of Maryland, Baltimore	Hepatitis B? Chronic\|Hepatitis C	December 2014
NCT04997564	Peking University First Hospital	Chronic Hepatitis C\|Chronic Hepatitis B	August 2021	Phase 4
NCT04034368	The First Hospital of Jilin University	HBV	August 2019	Phase 4
NCT05550519	Janssen Pharmaceutica N.V., Belgium	Hepatitis B, Chronic	October 31, 2022	Early Phase 1
NCT04065230	Southeast University, China	Hepatitis B Virus\|Mother to Child Transmission	August 2019
NCT04880577	Massachusetts General Hospital\|Gilead Sciences	Multiple Sclerosis, Relapsing-Remitting\|Fatigue	September 15, 2022	Phase 2
NCT04237376	New Discovery LLC	Hepatitis B, Chronic\|Pregnancy Related	April 9, 2019
NCT03640728	First Affiliated Hospital Xi´an Jiaotong University	Hepatitis B\|Virus Diseases\|Liver Failure	January 25, 2019
NCT03559790	The Catholic University of Korea	Chronic Hepatitis b	July 18, 2018
NCT04712058	National Taiwan University Hospital\|Far Eastern Memorial Hospital\|Mackay Memorial Hospital\|Changhua Christian Hospital\|Chung Shan Medical University\|National Cheng-Kung University Hospital\|Chi Mei Medical Hospital\|Kaohsiung Medical University Chung-Ho Memorial Hospital\|Kaohsiung Municipal Ta-Tung Hospital	HIV Infections	January 20, 2021	Not Applicable

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 93.55 mM ; Need ultrasonic)

H ₂ O : 20 mg/mL ( 37.42 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.8709 mL	9.3545 mL	18.7091 mL
5 mM	0.3742 mL	1.8709 mL	3.7418 mL
10 mM	0.1871 mL	0.9355 mL	1.8709 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: PBS

Solubility: 4.55 mg/mL (8.51 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (4.68 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: 2.5 mg/mL (4.68 mM); Clear solution; Need warming

* All of the co-solvents are available by MCE.

References

[1] Birkus G, et al. Intracellular Activation of Tenofovir Alafenamide and the Effect of Viral and Host Protease Inhibitors. Antimicrob Agents Chemother. 2015 Oct 26;60(1):316-22.
[2] Callebaut C, et al. In Vitro Virology Profile of Tenofovir Alafenamide, a Novel Oral Prodrug of Tenofovir with Improved Antiviral Activity Compared to That of Tenofovir Disoproxil Fumarate. Antimicrob Agents Chemother. 2015 Oct;59(10):5909-16.

Synonyms

L-Alanine, N-[(S)-[[(1R)-2-(6-amino-9H-purin-9-yl)-1-methylethoxy]methyl]phenoxyphosphinyl]-, 1-methylethyl ester, (2E)-2-butenedioate (2:1)

Tenofovir alafenamide fumarate

GS 7340-03

Tenofovir alafenamide hemifumarate

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