MDL | MFCD13188530 |
---|---|
Molecular Weight | 513.67 |
Molecular Formula | C29H41F2N5O |
SMILES | O=C(C1CCC(F)(F)CC1)N[C@H](C2=CC=CC=C2)CCN3[C@H]4C[C@@H](N5C(C)=NN=C5C(C)C)C[C@@H]3CC4 |
MIP-1α-CCR5 3.3 nM (IC 50 , in HEK-293 cell membrane) |
RANTES-CCR5 5.2 nM (IC 50 , in HEK-293 cell membrane) |
MIP-1β-CCR5 7.2 nM (IC 50 , in HEK-293 cell membrane) |
||
HIV-1 (Ba-L) 1.1 nM (IC 50 , in PM-1 cells) |
Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity. Maraviroc inhibits the downstream event of chemokine-induced intracellular calcium redistribution, with IC
50
s ranging from 7 to 30 nM obtained against MIP-1β, MIP-1α and RANTES.
Maraviroc (UK-427857) is active (IC
90
) at low nanomolar concentrations against HIV-1 Ba-L (a lab-adapted R5 strain) when measured in a 5-day antiviral assay using either isolated multiple (pooled) donor PBMC (IC
90
, 3.1 nM), single-donor PBMC (IC
90
, 1.8 nM) or PM-1 cells (IC
90
, 1.1 nM)
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clearance values are moderate to high in both rat and dog species following i.v. administration (74 and 21 mL/min/kg, respectively). Maraviroc also has a moderate volume of distribution in both species (4.3 to 6.5 liters/kg). The half-life values of maraviroc are 0.9 h in the rat and 2.3 h in the dog. Following oral administration (2 mg/kg) to the dog, the C max (256 ng/mL) occurs 1.5 h. post-dose, and the bioavailability is 40%. For the rat, investigation of the concentrations obtain in the portal vein following oral administration indicated that approximately 30% of the administered dose is absorbed from the intestinal tract [1] . In the DSS/TNBS colitis and in the transfer model, Maraviroc attenuates development of intestinal inflammation by selectively reducing the recruitment of CCR5 bearing leukocytes [2]
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
NCT Number | Sponsor | Condition | Start Date | Phase |
---|---|---|---|---|
NCT00098306 | ViiV Healthcare|Pfizer |
HIV Infections
|
November 2004 | Phase 2|Phase 3 |
NCT04435522 | Rhode Island Hospital |
COVID
|
October 1, 2020 | Phase 1 |
NCT02519777 | National Institute of Allergy and Infectious Diseases (NIAID) |
HIV Infections
|
April 21, 2016 | Phase 4 |
NCT01894776 | Ottawa Hospital Research Institute|Pfizer |
HIV Infection|HIV-1 Infection|Mycobacterium Avium Complex (MAC)
|
June 2013 | Phase 1 |
NCT01736813 | National Center for Tumor Diseases, Heidelberg|University Hospital Heidelberg |
Colorectal Cancer|Neoplasm Metastasis|Liver Metastases
|
November 2012 | |
NCT01140412 | ViiV Healthcare|Pfizer |
Healthy
|
July 2010 | Phase 1 |
NCT00944541 | French National Agency for Research on AIDS and Viral Hepatitis|Pfizer |
HIV Infection|HIV Infections
|
September 2009 | Phase 2 |
NCT01384682 | Kirby Institute|ViiV Healthcare|Pfizer |
HIV
|
August 2011 | Phase 4 |
NCT03274804 | University Hospital Heidelberg|Institut für Klinische Krebsforschung IKF GmbH am Krankenhaus Nordwest |
Metastatic Colorectal Cancer|MSS
|
April 1, 2018 | Phase 1 |
NCT02208037 | National Heart, Lung, and Blood Institute (NHLBI)|Blood and Marrow Transplant Clinical Trials Network|National Cancer Institute (NCI) |
Acute Leukemia|Chronic Myelogenous Leukemia|Myelodysplasia|Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma|Lymphoma, B-Cell|Lymphoma, Follicular|Lymphoma, Large B-Cell, Diffuse|Hodgkin´s Lymphoma
|
August 2014 | Phase 2 |
NCT00719823 | ViiV Healthcare|Pfizer |
Human Immunodeficiency Virus Type 1
|
August 2008 | Phase 3 |
NCT02741323 | National Institute of Allergy and Infectious Diseases (NIAID) |
HIV Infections|Kidney Diseases
|
January 1, 2017 | Phase 2 |
NCT02486510 | Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal |
HIV-1 Infection
|
July 2012 | Early Phase 1 |
NCT02167451 | Children´s Hospital Medical Center, Cincinnati |
Diagnoses That Require Stem Cell Transplant|Graft Versus Host Disease (GVHD)
|
July 2014 | Phase 1|Phase 2 |
NCT04789616 | University of Calgary|University Health Network, Toronto|University of California, Los Angeles|Sunnybrook Health Sciences Centre|University of British Columbia|Memorial University of Newfoundland|Dalhousie University|Parkwood Hospital, London, Ontario|Riverview Health Centre Foundation|The Dr. Miriam and Sheldon G. Adelson Medical Research Foundation |
Stroke
|
May 2022 | Phase 2 |
NCT00981773 | Imperial College London|Mater Misericordiae University Hospital |
HIV Infections
|
September 2009 | Phase 4 |
NCT00948753 | Abramson Cancer Center of the University of Pennsylvania |
Graft-versus-host Disease|Hematopoietic Stem Cell Transplantation
|
June 2009 | Phase 1|Phase 2 |
NCT03172026 | University of California, Los Angeles |
Stroke
|
August 1, 2019 | Phase 2|Phase 3 |
NCT05470491 | National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) |
HIV|Hematologic Malignancies
|
November 27, 2022 | Phase 1|Phase 2 |
NCT00870363 | University of California, Davis |
HIV Infections
|
April 2009 | Phase 4 |
NCT00808002 | Germans Trias i Pujol Hospital |
HIV Infections
|
February 2009 | Phase 3 |
NCT04965662 | Guy´s and St Thomas´ NHS Foundation Trust|ViiV Healthcare|Gilead Sciences |
HIV-1-infection
|
January 1, 2018 | Phase 4 |
NCT02475915 | South East Asia Research Collaboration with Hawaii|The Thai Red Cross AIDS Research Centre|Cooper Human Systems |
Acute HIV Infection
|
January 2015 | Phase 1|Phase 2 |
NCT01585753 | Kirby Institute |
Cardiovascular Disease
|
June 2012 | |
NCT00098748 | ViiV Healthcare|Pfizer |
HIV Infections
|
November 2004 | Phase 2|Phase 3 |
NCT00977756 | International Maternal Pediatric Adolescent AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) |
HIV Infections
|
August 2002 | |
NCT02990312 | University of Maryland, Baltimore |
Hiv|Kidney Transplant|HIV Reservoir|CCR5
|
May 1, 2017 | Phase 4 |
NCT00795444 | Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal|Pfizer |
HIV-1
|
March 2008 | Phase 2 |
NCT00844519 | University of California, San Francisco|National Heart, Lung, and Blood Institute (NHLBI)|Pfizer |
HIV Infection|Cardiovascular Disease|Inflammation|HIV Infections
|
January 2010 | Phase 3 |
NCT02346084 | International Partnership for Microbicides, Inc.|National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health (NIH) |
HIV+AIDS
|
January 2015 | Phase 1 |
NCT03163277 | Giovanni Di Perri|University of Turin, Italy |
Hiv|Neurocognitive Dysfunction
|
May 15, 2017 | Phase 4 |
NCT01980329 | Johns Hopkins University |
Cytochrome P450 CYP3A5 Enzyme Polymorphism|Healthy Subjects|Pharmacokinetics of Maraviroc
|
January 2013 | Phase 1 |
NCT04475991 | Hospital General de México Dr. Eduardo Liceaga|CCINSHAE. Secretaría de Salud. México|Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran|Centro de Investigación en. Enfermedades Infecciosas, Mexico |
COVID-19
|
July 13, 2021 | Phase 2 |
NCT00827112 | ViiV Healthcare|Pfizer |
Human Immunodeficiency Virus-1
|
March 2009 | Phase 2 |
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 | |
NCT01204905 | University of Maryland, Baltimore|Merck Sharp & Dohme LLC |
HIV Infections
|
September 2010 | Not Applicable |
NCT01068873 | Temple University|Abbott|Pfizer |
HIV Infections
|
April 2010 | Phase 4 |
NCT02934022 | Southern California Institute for Research and Education|Pfizer |
HIV Infection
|
June 2012 | Not Applicable |
NCT01680536 | St Stephens Aids Trust |
HIV
|
November 2012 | Phase 4 |
NCT00771823 | St Stephens Aids Trust |
HIV Infections
|
May 2008 | Phase 1 |
NCT00982878 | Imperial College London|Pfizer |
HIV Infections
|
September 2009 | Phase 1 |
NCT02961829 | Federal University of São Paulo|Fundação de Amparo à Pesquisa do Estado de São Paulo|Conselho Nacional de Desenvolvimento Científico e Tecnológico|ViiV Healthcare |
Chronic Infection|HIV
|
July 2015 | Not Applicable |
NCT01154673 | University of Toronto|Unity Health Toronto|Maple Leaf Research |
Acute HIV Infection
|
November 2011 | Phase 2|Phase 3 |
NCT00966329 | Germans Trias i Pujol Hospital |
HIV|HIV Infections
|
October 2009 | Phase 4 |
NCT00426660 | ViiV Healthcare |
HIV Infections
|
February 2007 | Phase 3 |
NCT01329783 | ViiV Healthcare|Copenhagen HIV Programme|Pfizer |
HIV|AIDS
|
April 2007 | |
NCT01363037 | International Partnership for Microbicides, Inc. |
HIV Infections
|
November 2011 | Phase 1 |
NCT01627717 | Centre hospitalier de l´Université de Montréal (CHUM)|Université de Montréal|McGill University Health Centre+Research Institute of the McGill University Health Centre|Toronto General Hospital |
Healthy
|
June 2012 | Phase 1 |
NCT00709111 | AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) |
HIV Infections
|
January 2009 | Not Applicable |
NCT01597648 | GlaxoSmithKline |
Infection, Human Immunodeficiency Virus I
|
November 2011 | Phase 1 |
NCT04710199 | Fundación Pública Andaluza para la gestión de la Investigación en Sevilla |
Virus Diseases
|
February 23, 2021 | Phase 2 |
NCT00976404 | Robert L. Murphy|Objectif Recherche Vaccins SIDA|National Institute of Allergy and Infectious Diseases (NIAID)|Pfizer|Merck Sharp & Dohme LLC|Northwestern University |
HIV Infection
|
November 2009 | Phase 2 |
NCT01133210 | Washington University School of Medicine|Pfizer |
Hypertriglyceridemia
|
January 2011 | Phase 1 |
NCT00791700 | ViiV Healthcare|Pfizer |
Human Immunodeficiency Virus
|
April 22, 2009 | Phase 2 |
NCT04721301 | University Hospital Heidelberg|German Cancer Research Center |
Colorectal Cancer Metastatic|Pancreatic Cancer Metastatic
|
January 15, 2017 | Phase 1 |
NCT01276236 | University of California, San Francisco|Pfizer|ViiV Healthcare |
Kaposi´s Sarcoma
|
March 9, 2011 | Phase 2 |
NCT00981318 | Rodwick, Barry M., M.D.|Abbott |
HIV Infections|Acquired Immunodeficiency Syndrome
|
December 2009 | Phase 4 |
NCT01597895 | ViiV Healthcare|Pfizer |
Healthy
|
July 2012 | Phase 1 |
NCT00884858 | ASST Fatebenefratelli Sacco |
HIV Infections
|
April 2009 | Phase 4 |
NCT03129113 | University College, London|Medical Research Council|ViiV Healthcare|Royal Free Hospital NHS Foundation Trust |
Hepatic Steatosis|HIV-1-infection
|
March 1, 2017 | Phase 2|Phase 3 |
NCT01348308 | ANRS, Emerging Infectious Diseases|Pfizer |
HIV-1 Infection|AIDS
|
September 2011 | Phase 3 |
NCT01013987 | Fundación Huésped|Pfizer |
HIV-1 Adults Patients|AIDS|Triple Class Failure
|
February 2010 | Phase 4 |
NCT00801515 | ViiV Healthcare|Pfizer |
HIV
|
August 2009 | |
NCT00925756 | University of California, San Diego|University of California, Los Angeles|University of Southern California|Pfizer|California HIV+AIDS Research Program |
HIV Infections
|
October 20, 2008 | Phase 4 |
NCT01389063 | S.F.L. van Lelyveld|UMC Utrecht |
Endothelial Dysfunction
|
January 2012 | Phase 4 |
NCT01242579 | International Partnership for Microbicides, Inc. |
HIV Infections
|
January 2011 | Phase 1 |
NCT00735072 | University of California, San Francisco|Pfizer|amfAR, The Foundation for AIDS Research|Stanford University|Case Western Reserve University|Rush University |
HIV Infection
|
September 2008 | Phase 4 |
NCT02480894 | ViiV Healthcare|GlaxoSmithKline |
Infection, Human Immunodeficiency Virus
|
July 7, 2015 | Phase 1 |
NCT00992654 | ViiV Healthcare|Pfizer |
Human Immunodeficiency Virus (HIV)
|
||
NCT00783484 | Pfizer |
Healthy Volunteers
|
October 2008 | Phase 1 |
NCT01190293 | St Stephens Aids Trust |
HIV Infection
|
January 2010 | Phase 4 |
NCT02134717 | Kevin F. Gibson|University of Pittsburgh |
Sarcoidosis
|
January 2014 | Not Applicable |
NCT02625207 | ViiV Healthcare|Pfizer |
Healthy Subjects
|
November 6, 2015 | Phase 1 |
NCT00643643 | ViiV Healthcare|Pfizer |
HIV Infections
|
October 2002 | Phase 2 |
NCT01505114 | National Institute of Allergy and Infectious Diseases (NIAID)|HIV Prevention Trials Network|AIDS Clinical Trials Group |
HIV Infection
|
June 2012 | Phase 2 |
NCT01637233 | Kirby Institute |
HIV-1 Infection
|
June 2012 | |
NCT01533272 | Hospital Clinic of Barcelona |
HIV Infection
|
February 2012 | Phase 4 |
NCT01785810 | Abramson Cancer Center of the University of Pennsylvania |
Hematologic Malignancy
|
February 2013 | Phase 2 |
NCT01049204 | St Stephens Aids Trust |
HIV Infections
|
July 2009 | Phase 4 |
NCT00665561 | ViiV Healthcare|Pfizer |
Human Immunodeficiency Virus
|
March 31, 2008 | |
NCT00853840 | ViiV Healthcare|Pfizer |
AIDS
|
April 2008 | Phase 4 |
NCT03178084 | Fundacion para la Investigacion Biomedica del Hospital Universitario Ramon y Cajal |
HIV+AIDS
|
October 15, 2014 | Phase 3 |
NCT04966429 | Tel-Aviv Sourasky Medical Center|Hadassah Medical Organization|Soroka University Medical Center |
Post Stroke Cognitive Impairment
|
May 1, 2021 | Phase 2 |
NCT02039323 | University of North Carolina, Chapel Hill |
Healthy Adult Females
|
February 2014 | Phase 1 |
NCT03402815 | University Of Perugia |
HIV Infection With Other Conditions|Cardiovascular Risk Factor|Atherosclerosis|Inflammation
|
January 1, 2015 | Phase 4 |
NCT01327547 | ViiV Healthcare|Pfizer |
HIV Coinfection
|
May 18, 2011 | Phase 4 |
NCT00782301 | ViiV Healthcare|Pfizer |
Hepatitis B|Human Immunodeficiency Virus|Hepatitis C, Chronic
|
March 2009 | Phase 4 |
NCT00537394 | National Institute of Allergy and Infectious Diseases (NIAID)|AIDS Clinical Trials Group |
HIV Infections
|
January 2008 | Phase 3 |
NCT00634959 | ViiV Healthcare|Pfizer |
HIV
|
July 2003 | Phase 2 |
NCT00666705 | ViiV Healthcare|Pfizer |
Healthy
|
February 2008 | Phase 4 |
NCT01896921 | University of Maryland, Baltimore |
HIV
|
September 2013 | Phase 3 |
NCT00496782 | ViiV Healthcare|Pfizer |
HIV Infections
|
July 2007 | Phase 1 |
NCT03708861 | University of Turin, Italy |
HIV Infection
|
January 2016 | Phase 3 |
NCT00988780 | Instituto Nacional de Ciencias Medicas y Nutricion Salvador Zubiran|University of Witwatersrand, South Africa|Case Western Reserve University|The Wistar Institute|University of Pennsylvania |
Immune Reconstitution Inflammatory Syndrome|HIV|HIV Infections
|
December 2009 | Not Applicable |
NCT01866267 | St. Hope Foundation|GlaxoSmithKline |
Human Immunodeficiency Virus|AIDS
|
January 2013 | Phase 4 |
NCT03218592 | University of North Carolina, Chapel Hill|National Institute of Allergy and Infectious Diseases (NIAID) |
HIV+AIDS
|
June 28, 2017 | Phase 4 |
NCT00098722 | ViiV Healthcare|Pfizer |
HIV Infections
|
December 2004 | Phase 2|Phase 3 |
NCT01749566 | Emory University |
HIV
|
December 2012 | Phase 1 |
NCT02881762 | University of Maryland, Baltimore|ViiV Healthcare |
Hepatitis C|Human Immunodeficiency Virus
|
June 1, 2017 | Phase 4 |
NCT01235013 | Hospital Clinic of Barcelona |
HIV-1 Infection
|
Phase 4 | |
NCT01637259 | Kirby Institute |
Proteinuria|HIV
|
June 2012 | Phase 4 |
NCT02333045 | Emory University |
HIV
|
January 2015 | Not Applicable |
NCT01348763 | Imperial College London |
HIV
|
October 2011 | Phase 1 |
NCT00987948 | University of Hawaii|Pfizer |
HIV Infections
|
January 2010 | Phase 2 |
NCT01290211 | ViiV Healthcare|Pfizer |
Healthy
|
April 2011 | Phase 1 |
NCT04441385 | Hospital Universitario Infanta Leonor|Hospital Clinic of Barcelona|ViiV Healthcare |
COVID-19
|
June 26, 2020 | Phase 2 |
NCT00717067 | ViiV Healthcare|Pfizer |
Human Immunodeficiency Virus (HIV) Infection
|
July 2008 | Phase 4 |
NCT01449006 | Bruce Brew|ViiV Healthcare|St Vincent´s Hospital, Sydney |
Human Immunodeficiency Virus (HIV)|HIV Associated Neurocognitive Disorders (HAND)
|
October 2011 | Phase 4 |
NCT01060618 | Asociacion para el Estudio de las Enfermedades Infecciosas |
HIV Infections
|
May 2009 | Phase 2|Phase 3 |
NCT02159027 | University of Hawaii|ViiV Healthcare|University of Puerto Rico |
AIDS Dementia Complex
|
June 2015 | Phase 2|Phase 3 |
NCT02799888 | Affiliated Hospital to Academy of Military Medical Sciences |
Graft-versus-host Disease|Hematopoietic Stem Cell Transplantation
|
April 2014 | Phase 2 |
NCT00098293 | ViiV Healthcare|Pfizer |
HIV-1
|
November 2004 | Phase 3 |
NCT00875368 | S.F.L. van Lelyveld|Academisch Medisch Centrum - Universiteit van Amsterdam (AMC-UvA)|Erasmus Medical Center|Leiden University Medical Center|Onze Lieve Vrouwe Gasthuis|Slotervaart Hospital|Rijnstate Hospital|Pfizer|UMC Utrecht |
HIV Infections
|
February 2009 | Phase 4 |
NCT01400412 | AIDS Clinical Trials Group|National Institute of Allergy and Infectious Diseases (NIAID) |
HIV-1 Infection
|
January 17, 2012 | Phase 2 |
NCT00775294 | University of North Carolina, Chapel Hill|Pfizer |
HIV+AIDS
|
May 2008 | Phase 1 |
NCT01719627 | Fundación FLS de Lucha Contra el Sida, las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia |
HIV
|
October 2012 | Phase 1 |
NCT01345630 | ViiV Healthcare|Pfizer |
HIV-1
|
September 2011 | Phase 3 |
NCT00821535 | ViiV Healthcare|Pfizer |
Human Immunodeficiency Virus (HIV) Infection
|
February 2009 | Phase 1 |
NCT00427934 | Pfizer |
Arthritis, Rheumatoid
|
February 2007 | Phase 2 |
NCT01428986 | National Center for Global Health and Medicine, Japan |
HIV Infections|AIDS
|
November 2009 | |
NCT00850395 | ViiV Healthcare|Pfizer |
HIV-1
|
July 2009 | |
NCT00764465 | Garden State Infectious Disease Associates, PA|GlaxoSmithKline |
Healthy
|
October 2008 | Phase 2 |
NCT00703586 | Rockefeller University|Aaron Diamond AIDS Research Center|Pfizer |
HIV Infections
|
September 2007 | Phase 1 |
NCT00993148 | Northwestern University|Pfizer|Tibotec, Inc |
HIV-1 Infection|HIV Infections
|
May 2010 | Phase 2 |
NCT01056874 | ViiV Healthcare|Pfizer |
Healthy|HIV Infections
|
March 2010 | Phase 1 |
NCT02778204 | National Institute of Allergy and Infectious Diseases (NIAID)|Eunice Kennedy Shriver National Institute of Child Health and Human Development (NICHD)|ViiV Healthcare|GlaxoSmithKline |
HIV Infections
|
June 5, 2017 | Phase 1 |
NCT00478231 | ViiV Healthcare|Pfizer |
Acquired Immunodeficiency Syndrome|HIV Infection
|
July 2007 | Phase 3 |
NCT00525733 | Rockefeller University|Aaron Diamond AIDS Research Center|Merck Sharp & Dohme LLC|Pfizer |
HIV Infections
|
October 2007 | Not Applicable |
Solid
Room temperature in continental US; may vary elsewhere.
Powder | -20°C | 3 years |
---|---|---|
4°C | 2 years | |
In solvent | -80°C | 6 months |
-20°C | 1 month |
DMSO : 50 mg/mL ( 97.34 mM ; Need ultrasonic)
Ethanol : 6.5 mg/mL ( 12.65 mM ; Need ultrasonic)
Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
---|
1 mM | 1.9468 mL | 9.7339 mL | 19.4678 mL |
5 mM | 0.3894 mL | 1.9468 mL | 3.8936 mL |
10 mM | 0.1947 mL | 0.9734 mL | 1.9468 mL |
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution
Add each solvent one by one: 1% DMSO >> 99% saline
Solubility: ≥ 0.5 mg/mL (0.97 mM); Clear solution