|3-氯-5-((1-((4-甲基-5-氧代-4,5-二氢-1H-1,2,4-三唑-3-基)甲基)-2-氧代-4-(三氟甲基)-1,2-二氢吡啶-3-基)氧基)苯甲腈|CsnPharm

CAS No.: 1338225-97-0

Doravirine/多拉维林 Catalog No. CSN18664

Synonyms: MK-1439;Pifeltro;多拉维林

Doravirine is a non-nucleoside inhibitor of HIV-1 reverse transcriptase with potent activity against wild-type virus (95% inhibitory concentration 19 nM, 50% human serum).

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实验方案

技术信息

生物活性

描述Doravirine (MK-1439) is a highly specific HIV-1 nonnucleoside reverse transcriptase inhibitor with IC50s of 12, 9.7 and 9.7nM against the wild type and K103N and Y181C reverse transcriptase mutants, respectively. Selectivity and cytotoxicity studies confirmed that Doravirine is a highly specific nonnucleoside reverse transcriptase inhibitor with minimum off-target activities. In the presence of 50% normal human serum (NHS), Doravirine shows excellent potency in suppressing the replication of WT virus, with a 95% effective concentration (EC95) of 20 nM, as well as K103N, Y181C, and K103N/Y181C mutant viruses with EC9595 of 43, 27, and 55 nM, respectively^[3]. Doravirine exhibits similar antiviral activities against 10 different HIV-1 subtype viruses (a total of 93 viruses). Administration of 50 mg Doravirine with a high-fat meal is associated with slight elevations in AUC time zero to infinity and C24 h with no change in Cmax^[4].
临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02397096	HIV-1 Infection	Phase 3	Active, not recruiting	November 2, 2021	-
NCT02629822	HIV-1 Infection	Phase 2	Active, not recruiting	October 29, 2020	-
NCT02652260	HIV-1 Infection ... more >> CNS Toxicity Collapse <<	Phase 2	Active, not recruiting	June 18, 2020	-

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参考文献

[1] Feng M, Sachs NA, et al. Doravirine Suppresses Common Nonnucleoside Reverse Transcriptase Inhibitor-Associated Mutants at Clinically Relevant Concentrations. Antimicrob Agents Chemother. 2016 Mar 25;60(4):2241-7.
[2] Lai MT, Feng M, et al. In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2014;58(3):1652-63.
[3] Lai MT, Feng M, Falgueyret JP, et al. In vitro characterization of MK-1439, a novel HIV-1 nonnucleoside reverse transcriptase inhibitor. Antimicrob Agents Chemother. 2014;58(3):1652-1663.
[4] Anderson MS, Gilmartin J, Cilissen C, et al. Safety, tolerability and pharmacokinetics of doravirine, a novel HIV non-nucleoside reverse transcriptase inhibitor, after single and multiple doses in healthy subjects. Antivir Ther. 2015;20(4):397-405.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3488 mL
- 11.7440 mL
- 23.4880 mL
- 5 mM
- 0.4698 mL
- 2.3488 mL
- 4.6976 mL
- 10 mM
- 0.2349 mL
- 1.1744 mL
- 2.3488 mL

技术信息

CAS号

1338225-97-0

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H11ClF3N5O3

运输

蓝冰

分子量

425.75

别名

MK-1439;Pifeltro;多拉维林

溶解度

DMSO	85.0 mg/mL (199.6 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02397096	HIV-1 Infection	Phase 3	Active, not recruiting	November 2, 2021	-
NCT02629822	HIV-1 Infection	Phase 2	Active, not recruiting	October 29, 2020	-
NCT02652260	HIV-1 Infection ... more >> CNS Toxicity Collapse <<	Phase 2	Active, not recruiting	June 18, 2020	-
NCT02403674	Human Immunodeficiency Virus (... more >>HIV) Collapse <<	Phase 3	Active, not recruiting	November 5, 2021	-
NCT02549040	Human Immunodeficiency Virus-1... more >> (HIV-1) Collapse <<	Phase 1	Completed	-	-
NCT02403674	-	-	Active, not recruiting	-	-
NCT01466985	HIV-1 Infection	Phase 1	Completed	-	-
NCT03332095	HIV Infections	Phase 1 Phase 2	Recruiting	October 2021	United States, Colorado ... more >> Univ. of Colorado Denver NICHD CRS Recruiting Aurora, Colorado, United States, 80045 Contact: Emily Barr, C.P.N.P., C.N.M., M.S.N. 720-777-6752 emily.barr@childrenscolorado.org United States, Florida Univ. of Florida Jacksonville NICHD CRS Recruiting Jacksonville, Florida, United States, 32209 Contact: Saniyyah Mahmoudi, A.R.N.P. 904-244-5331 saniyyah.mahmoudi@jax.ufl.edu United States, Maryland Johns Hopkins Univ. Baltimore NICHD CRS Recruiting Baltimore, Maryland, United States, 21287 Contact: Aleisha Collinson-Streng, R.N., A.C.R.N. 443-801-7301 acolli14@jhmi.edu United States, Massachusetts Boston Medical Center Ped. HIV Program NICHD CRS Recruiting Boston, Massachusetts, United States, 02118 Contact: Debra McLaud, R.N. 617-414-5813 demclaud@bmc.org United States, Tennessee St. Jude Children's Research Hospital CRS Recruiting Memphis, Tennessee, United States, 38105-3678 Contact: Sandra Jones, P.N.P. 901-595-5059 Sandra.Jones2@STJUDE.org United States, Washington Seattle Children's Research Institute CRS Recruiting Seattle, Washington, United States, 98101 Contact: Amanda Robson Nuss, B.S. 206-884-1535 amanda.robson@seattlechildrens.org Puerto Rico University of Puerto Rico Pediatric HIV/AIDS Research Program CRS Recruiting San Juan, Puerto Rico, 00935 Contact: Ruth Santos, B.S.N., R.N., M.P.H. 787-759-9595 ruth.santos@upr.edu Thailand Siriraj Hospital ,Mahidol University NICHD CRS Recruiting Bangkok, Bangkoknoi, Thailand, 10700 Contact: Watcharee Lermankul 66-2-4197000 ext 5695 watchareeped@gmail.com Collapse <<
NCT02089659	HIV-1 Infection	Phase 1	Completed	-	-
NCT02275780	HIV-1	Phase 3	Active, not recruiting	June 23, 2021	-
NCT03272347	HIV-1 Infection	Phase 2	Active, not recruiting	September 29, 2020	United States, Arizona ... more >> Pueblo Family Physicians ( Site 0119) Phoenix, Arizona, United States, 85015 United States, California University California / Davis ( Site 0101) Sacramento, California, United States, 95817 United States, District of Columbia Whitman Walker Clinic ( Site 0108) Washington, District of Columbia, United States, 20005 United States, Florida Orlando Immunology Center (OIC) ( Site 0105) Orlando, Florida, United States, 32803 United States, Illinois Northstar Medical Center ( Site 0102) Chicago, Illinois, United States, 60657 United States, Missouri Kansas City CARE Clinic ( Site 0106) Kansas City, Missouri, United States, 64111 United States, Texas Saint Hope Foundation, Inc. ( Site 0116) Bellaire, Texas, United States, 77401 North Texas Infectious Diseases Consultants, PA ( Site 0103) Dallas, Texas, United States, 75246 Tarrant County Infectious Disease Associates ( Site 0112) Fort Worth, Texas, United States, 76104 The Crofoot Research Center, Inc. ( Site 0118) Houston, Texas, United States, 77098 Chile Clinica Arauco Salud ( Site 0200) Santiago, RM, Chile Biomedica Research Group ( Site 0202) Santiago, Chile Hospital Dr. Hernan Henriquez Aravena ( Site 0203) Temuco, Chile France Hopital Avicenne ( Site 2302) Bobigny, France Hopital Saint-Andre ( Site 2307) Bordeaux, France CHU Hotel Dieu ( Site 2308) Nantes, France CHU de Nice Hopital Archet 1 ( Site 2303) Nice, France Hopital Bichat - Claude Bernard ( Site 2309) Paris, France Hopital Pitie Salpetriere ( Site 2305) Paris, France Hopital Saint Louis ( Site 2306) Paris, France Centre Hospitalier de Tourcoing ( Site 2301) Tourcoing, France United Kingdom Brighton and Sussex University Hospitals NHS Trust ( Site 2105) Brighton, East Sussex, United Kingdom Chelsea and Westminster Hospital ( Site 2101) London, United Kingdom Royal London Hospital ( Site 2103) London, United Kingdom The Royal Free London NHS Foundation Trust ( Site 2102) London, United Kingdom North Manchester General Hospital ( Site 2104) Manchester, United Kingdom Collapse <<
NCT02641067	Renal Impairment	Phase 1	Completed	-	-
NCT01632345	-	-	Completed	-	-
NCT02275780	-	-	Active, not recruiting	-	-
NCT01632345	HIV Infections	Phase 2	Completed	-	-
NCT02715700	Human Immunodeficiency Virus (... more >>HIV) Infection Collapse <<	Phase 1	Completed	-	-

Doravirine/多拉维林 Catalog No. CSN18664

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