|(2R,5S,13aR)-8-羟基-7,9-二氧代-N-(2,4,6-三氟苄基)-2,3,4,5,7,9,13,13a-八氢-2,5-甲基吡啶[1',2':4,5]吡嗪[2,1-b][1,3]恶嗪-10-甲酰胺|CsnPharm

CAS No.: 1611493-60-7

(2R,5S,13aR)-8-Hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide Catalog No. CSN20343

Synonyms: GS-9883;GS-988301

Bictegravir is a potent, unboosted, once-Daily HIV-1 Integrase Strand Transfer inhibitor (INSTI) (IC50 - 1.6 nM) with improved pharmacokinetics and in vitro resistance profile.

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生物活性

实验方案

技术信息

生物活性

描述Unique among animal viruses is the requirement for retroviruses to integrate their genetic information into the genome of the host cell that they infect. Integration is mediated by the viral protein integrase (IN), which is incorporated into fledgling viral particles alongside the other viral enzymes reverse transcriptase (RT) and protease (PR)^[4]. Bictegravir (BIC), a novel, potent, once-daily, unboosted inhibitor of HIV-1 integrase (IN), specifically targets IN strand transfer activity with IC₅₀ of 7.5 ± 0.3 nM and HIV-1 integration in cells^[5]. BIC exhibits potent and selective in vitro antiretroviral activity in both T-cell lines and primary human T lymphocytes, with EC₅₀s ranging from 1.5 to 2.4 nM and selectivity indices up to 8,700 relative to cytotoxicity. BIC displayed an in vitro resistance profile that was markedly improved compared to the integrase strand transfer inhibitors (INSTIs) raltegravir (RAL) and elvitegravir (EVG), and comparable to that of dolutegravir (DTG), against nine INSTI-resistant site-directed HIV-1 mutants. BIC displayed statistically improved antiviral activity relative to EVG, RAL, and DTG against a panel of 47 patient-derived HIV-1 isolates with high-level INSTI resistance. A high barrier to in vitro resistance emergence for BIC was also observed in viral breakthrough studies in the presence of constant clinically relevant drug concentrations^[5].

动物研究

剂量

Male Cynomolgus Monkey^[3]: 0.5 mg/kg (i.v.); 1 mg/kg (p.o.)

给药途径

i.v., p.o.

动物药代数据

Animal	Monkeys^[3]
Dose	0.5 mg/kg (i.v.) 1 mg/kg (p.o.)
Administration	i.v. p.o.
MRT	4.16 ± 0.93 h (i.v.)
F	73.8 ± 40.3 h (p.o.)
T_1/2	3.58 ± 0.23 h (i.v.) 3.26 ± 0.50 h (p.o.)
T_max	0.55 ± 0.06 h (i.v.) 0.83 ± 0.29 h (p.o.)
AUC_inf	49400 ± 12400 μM·h (i.v.) 72500 ± 39500 μM·h (p.o.)
CL	0.024 ± 0.007 L/h/kg (i.v.)
C_max	11500 ± 173 μM (i.v.) 16600 ± 4540 μM (p.o.)
AUC_last	49000 ± 12200 μM·h (i.v.) 72100 ± 39300 μM·h (p.o.)
Vss	0.095 ± 0.010 L/kg (i.v.)

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
NCT03472326	HIV-1-infection	Phase 2	Active, not recruiting	August 2020	Uganda ... more >> Joint Clinical Research Centre Kampala, Uganda, 10005 Collapse <<
NCT02652624	HIV-1 Infection	Phase 3	Active, not recruiting	November 2018	-
NCT03696160	HIV/AIDS	Phase 3	Not yet recruiting	July 2022	-

更多
参考文献

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
- 2.2253 mL
- 11.1264 mL
- 22.2529 mL
- 5 mM
- 0.4451 mL
- 2.2253 mL
- 4.4506 mL
- 10 mM
- 0.2225 mL
- 1.1126 mL
- 2.2253 mL

技术信息

CAS号

1611493-60-7

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

C21H18F3N3O5

运输

蓝冰

分子量

449.38

别名

GS-9883;GS-988301

溶解度

DMSO	87.0 mg/mL (193.6 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

NCT03472326	HIV-1-infection	Phase 2	Active, not recruiting	August 2020	Uganda ... more >> Joint Clinical Research Centre Kampala, Uganda, 10005 Collapse <<
NCT02652624	HIV-1 Infection	Phase 3	Active, not recruiting	November 2018	-
NCT03696160	HIV/AIDS	Phase 3	Not yet recruiting	July 2022	-
NCT03711253	Acute HIV Infection	Phase 4	Not yet recruiting	November 2021	United States, California ... more >> LA County-USC Medical Center Emergency Department Not yet recruiting Los Angeles, California, United States, 90033 Contact: Michael Menchine, MD Rand Schrader Health and Research Clinic Los Angeles, California, United States, 90033 Collapse <<
NCT03502005	Human Immunodeficiency Virus	Phase 4	Recruiting	September 2019	United States, Florida ... more >> Midland Research Group, Inc Recruiting Oakland Park, Florida, United States, 33334 Contact: Fletcher Neale 954-375-1275 fneale@midlandresearchgroup.com Contact: Clinical Research Coordinator Principal Investigator: Noah Lee, DO Sub-Investigator: Erik Lowman, DO Collapse <<
NCT03532425	HIV-1-infection	Phase 4	Recruiting	January 2020	Canada, Alberta ... more >> University of Alberta Recruiting Edmonton, Alberta, Canada, T6G 2B7 Contact: Stephen D Shafran, MD 780-407-6945 sshafran@ualberta.ca Collapse <<
NCT03739866	HIV-1 Infection	Phase 1	Recruiting	March 2020	United States, California ... more >> Ruane Clinical Research Group, Inc. Not yet recruiting Los Angeles, California, United States, 90036 United States, Florida Midway Immunology and Research Center Recruiting Fort Pierce, Florida, United States, 34982 Orlando Immunology Center Not yet recruiting Orlando, Florida, United States, 32803-1851 Triple O Research Institute, P.A. Recruiting West Palm Beach, Florida, United States, 33401 United States, Michigan Be Well Medical Center Recruiting Berkley, Michigan, United States, 48072-3436 United States, Texas AIDS Arms, Inc., DBA Prism Health North Texas Recruiting Dallas, Texas, United States, 75208 North Texas Infectious Diseases Consultants, P.A. Recruiting Dallas, Texas, United States, 75246 Tarrant County Infectious Disease Associates Not yet recruiting Fort Worth, Texas, United States, 76104 The Crofoot Research Center, INC (dba Gordon E. Crofoot MD PA) Recruiting Houston, Texas, United States, 77098 Collapse <<
NCT02603120	HIV-1 Infection	Phase 3	Active, not recruiting	June 2020	-
NCT02652624	-	-	Active, not recruiting	-	-
NCT02603107	HIV-1 Infection	Phase 3	Active, not recruiting	July 2020	-
NCT03348163	HIV Infections	Phase 4	Recruiting	April 1, 2020	United States, Texas ... more >> Thomas Street Health Center Recruiting Houston, Texas, United States, 77009 Contact: Anastasia Teper, MA 713-500-6797 Anastasia.Teper@uth.tmc.edu Collapse <<
NCT02603107	-	-	Active, not recruiting	-	-
NCT02881320	HIV-1 Infection	Phase 2 Phase 3	Active, not recruiting	November 2020	United States, Florida ... more >> Fort Pierce, Florida, United States, 34982 Jacksonville, Florida, United States, 32209 Tampa, Florida, United States, 33606 United States, Georgia Atlanta, Georgia, United States, 30322 United States, Michigan Detroit, Michigan, United States, 48201 United States, New York New York, New York, United States, 10016 United States, North Carolina Durham, North Carolina, United States, 27710 United States, Pennsylvania Philadelphia, Pennsylvania, United States, 19134 United States, Tennessee Memphis, Tennessee, United States, 38105 South Africa Bloemfontein, South Africa, 9301 Cape Town, South Africa, 7505 Cape Town, South Africa, 7646 Dundee, South Africa, 3000 Durban, South Africa, 4302 Johannesburg, South Africa, 2112 Pretoria, South Africa, 0089 Soweto, South Africa, 2013 Thailand Bangkok, Thailand, 10330 Bangkok, Thailand, 10700 Khon Kaen, Thailand, 40002 Uganda Kampala, Uganda Collapse <<
NCT02607956	HIV-1 Infection	Phase 3	Active, not recruiting	August 2020	-
NCT03631732	HIV-1 Infection	Phase 3	Recruiting	August 2020	-
NCT02607956	-	-	Active, not recruiting	-	-
NCT03547908	HIV-1/HBV Co-Infection	Phase 3	Recruiting	August 2023	-
NCT03110380	HIV-1-infection	Phase 3	Active, not recruiting	December 2020	-
NCT02607930	-	-	Active, not recruiting	-	-
NCT02397694	HIV-1 Infection	Phase 2	Active, not recruiting	January 2019	United States, Arizona ... more >> Phoenix, Arizona, United States, 85012 United States, California Los Angeles, California, United States, 90036 Los Angeles, California, United States, 90069 Sacramento, California, United States, 95817 United States, District of Columbia Washington, District of Columbia, United States, 20005 Washington, District of Columbia, United States, 20009 Washington, District of Columbia, United States, 20036 United States, Florida Fort Lauderdale, Florida, United States, 33316 Orlando, Florida, United States, 32803 West Palm Beach, Florida, United States, 33401 United States, Georgia Atlanta, Georgia, United States, 30312 Decatur, Georgia, United States, 30033 United States, Massachusetts Boston, Massachusetts, United States, 02115 United States, Michigan Berkley, Michigan, United States, 48072 United States, New Jersey Newark, New Jersey, United States, 07102 United States, Texas Austin, Texas, United States, 78705 Dallas, Texas, United States, 75208 Houston, Texas, United States, 77004 Houston, Texas, United States, 77098 Longview, Texas, United States, 75605 United States, Virginia Annandale, Virginia, United States, 22003 United States, Washington Seattle, Washington, United States, 98104 Collapse <<
NCT03656783	HIV	Phase 3	Not yet recruiting	November 30, 2020	United States, Massachusetts ... more >> Tufts Medical Center Not yet recruiting Boston, Massachusetts, United States, 02111 Contact: Laura Kogelman, MD lkogelman@tuftsmedicalcenter.org Contact: Deirdre Burke DBurke1@tuftsmedicalcenter.org Boston Medical Center Not yet recruiting Boston, Massachusetts, United States, 02118 Contact: Nina Lin, MD Nina.LIn@bmc.org Contact: Kristin Brierley Kristin.Brierley@bmc.org Collapse <<
NCT02607930	HIV-1 Infection	Phase 3	Active, not recruiting	April 2020	-
NCT03580668	-	-	Recruiting	November 2021	Canada ... more >> Clinique Medicale du Quartier Latin Recruiting Montréal, Canada, H2L 4E9 University of Ottawa Active, not recruiting Ottawa, Canada, K1N 6N5 St. Clair Medical Association/Balmoral Clinic Recruiting Toronto, Canada, M4T3A7 Collapse <<
NCT02400307	HIV	Phase 1	Completed	-	United States, Florida ... more >> Avail Clinical Research DeLand, Florida, United States, 32720 Clinical Pharmacology of Miami, Inc. Miami, Florida, United States, 33014-3616 Orlando Clinical Research Center Orlando, Florida, United States, 32809 United States, Minnesota Prism Clinical Research St. Paul, Minnesota, United States, 55114 United States, Tennessee New Orleans Center for Clinical Research Knoxville, Tennessee, United States, 37920 New Zealand Auckland Clinical Studies Limited Grafton, Auckland, New Zealand, 1010 Christchurch Clinical Studies Trust Christchurch, New Zealand, 8011 Collapse <<
NCT03405935	HIV-1-infection	Phase 3	Active, not recruiting	May 2020	Belgium ... more >> CHU Saint-Pierre Brussels, Belgium, 1000 UZ Gent Ghent, Belgium, 9000 France CHU Bordeaux - Groupe Hospitalier Sud Bordeaux, France, 33064 Hopital Saint-Andre Bordeaux, France, 33075 Hopital Europeen Marseille Marseille, France, 13006 C.H.U. de Nantes - Hotel Dieu Nantes, France, 44093 CHU de Nice Nice, France, 6203 Hopital Saint Louis PARIS cedex 10, France, 75475 Hopital Necker - Enfants Malades Paris, France, 75015 Hopital Saint Antoine Paris, France, 75571 CH de Tourcoing Tourcoing, France, 59208 Italy ASST Papa Giovanni XXIII Bergamo, Italy, 24127 ASST - Fatebenefratelli Sacco Milano, Italy, 20157 P.O. Spirito Santo - U.O. Malattie Infettive e Tropicali Pescara, Italy, 65124 IRCCS Istituto Nazionale per le Malattie Infettive Lazzaro Spallanzani Roma, Italy, 00149 Spain Hospital Universitari Germans Trias i Pujol Badalona, Spain, 8916 Hospital de la Santa Creu i Sant Pau Barcelona, Spain, 08026 Hospital Universitari Vall d'Hebron Barcelona, Spain, 08035 Hospital Clinic de Barcelona Barcelona, Spain, 08036 Hospital General Universitario Gregorio Maranon Madrid, Spain, 28007 Hospital Universitario Ramon y Cajal Madrid, Spain, 28034 Hospital Universitario 12 de Octubre Madrid, Spain, 28041 Hospital Universitario La Paz Madrid, Spain, 28046 Hospital Costa Del Sol Marbella, Spain, 29603 United Kingdom Newcastle Upon Tyne Hospitals NHS Foundation Trust Newcastle Upon Tyne, United Kingdom, NE1 4LP Collapse <<
NCT02603120	-	-	Active, not recruiting	-	-
NCT03499483	HIV Prevention	Phase 4	Not yet recruiting	September 1, 2021	-
NCT02275065	HIV-1 Infection	Phase 1	Completed	-	United States, California ... more >> Berkeley, California, United States Davis, California, United States Long Beach, California, United States Los Angeles, California, United States San Francisco, California, United States United States, District of Columbia Washington, District of Columbia, United States United States, Florida Fort Lauderdale, Florida, United States Orlando, Florida, United States Vero Beach, Florida, United States West Palm Beach, Florida, United States United States, Georgia Atlanta, Georgia, United States United States, Michigan Berkley, Michigan, United States United States, New Jersey Newark, New Jersey, United States United States, New Mexico Santa Fe, New Mexico, United States United States, Texas Dallas, Texas, United States United States, Washington Seattle, Washington, United States Collapse <<
NCT02397694	-	-	Active, not recruiting	-	-

(2R,5S,13aR)-8-Hydroxy-7,9-dioxo-N-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide Catalog No. CSN20343

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