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Cell Cycle/DNA DamageAntibody-drug Conjugate/ADC Related-
Methotrexate ????????????????????????????????????????????????????????? B ???????????????????????????????????????????????????????????????IC50??? 78 nM???
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生物活性
Description
Methotrexate is a traditionalfolateantagonist, with medianIC50of 78 nM for a 120 h drug exposure in a panel of six pediatric leukemia and lymphoma cell lines using the sulforhodamine B assay.
IC50& Target
Antifolate[1]
In Vitro
Methotrexate (MTX), which has a more predictable toxicity profile than aminopterin, has become a cornerstone of the treatment for childhood acute lymphoblastic leukemia (ALL) and for non-Hodgkins lymphoma[1].
In Vivo
Methotrexate (MTX) exposure reduces thymus and spleen indices of mice. Methotrexate markedly decreases white blood cells, thymic and splenic lymphocytes at dose ???5 mg/kg. However, there is a significant difference between the treatment plus control group and the model group (p<0.01). The combination of grape seed proanthocyanidins and Siberian ginseng eleutherosides obviously diminishes the effects of Methotrexate exposure on indices of thymus and spleens in mice[2].
Clinical Trial
KEMRI-Wellcome Trust Collaborative Research Program-University of Oxford
Malaria
March 2009
Phase 1
Baylor College of Medicine-Texas Children's Cancer Center
Cancer
December 2013
University Hospital, Rouen
ALOPECIA AREATA
February 2014
Phase 3
Amneal Pharmaceuticals, LLC-Accutest Research Laboratories (I) Pvt. Ltd.
Psoriasis-Rheumatoid Arthritis
August 2016
Phase 1
Astellas Pharma Global Development, Inc.-Basilea Pharmaceutica International Ltd-Astellas Pharma Inc
Pharmacokinetics of Isavuconazole-Pharmacokinetics of Methotrexate-Pharmacokinetics of 7-hydroxymethotrexate-Healthy Subjects
February 2013
Phase 1
Wake Forest University-Wake Forest University Health Sciences
Diabetic Macular Edema
September 2011
University of Nebraska
Rheumatoid Arthritis
January 2001
Phase 3
University of Pennsylvania-Bill and Melinda Gates Foundation
Ectopic Pregnancy
March 2001
Phase 3
Prof. Arie Levine-Wolfson Medical Center
Crohn's Disease
July 2015
Phase 4
Edward Averbukh-Hadassah Medical Organization
Central Serous Chorioretinopathy
August 2012
Phase 2
Universita degli Studi di Catania
Low Dose Methotrexate in Severe Chronic Asthma
February 2017
Phase 3
Children's Hospital of Philadelphia-The Leukemia and Lymphoma Society
Cancer-Leukemia-Lymphoma
May 2010
Phase 2
University Hospital, Strasbourg, France
Rheumatoid Arthritis-Insufficient Response to Methotrexate.
March 2016
Phase 4
Chonnam National University Hospital-Consortium for Improving Survival of Lymphoma
DLBCL
July 1, 2017
Phase 3
Central South University
Psoriasis Vulgaris
December 2015
Phase 2
University of North Carolina, Chapel Hill-Patient-Centered Outcomes Research Institute-ImproveCareNow (ICN)-The Leona M. and Harry B. Helmsley Charitable Trust-Children's Hospital Medical Center, Cincinnati-Grifols Diagnostics Solutions, Inc-National Institute of Arthritis and Musculoskeletal and Skin Diseases (NIAMS)-National Institutes of Health (NIH)
Pediatric Crohn's Disease
October 2016
Phase 3
Barnsley Hospital
Urticaria
August 2003
Phase 2
Tel-Aviv Sourasky Medical Center
To Evaluate the Effect of Therapy With IT MTX on the Disease Course of Patients With Progressive MS
January 2016
Early Phase 1
Georgetown University
Type 1 Diabetes Mellitus
February 1990
Instituto de Cardiologia do Rio Grande do Sul-Instituto de Cardiologia de Santa Catarina
Myocardial Infarction
April 2013
Phase 2
University of Western Ontario, Canada-Schering-Plough
Crohn's Disease
December 2005
Phase 3
City of Hope Medical Center-National Cancer Institute (NCI)
Leptomeningeal Metastases
September 2012
M.D. Anderson Cancer Center
Brain Tumor-Malignant Neoplasm of Fourth Ventricle of Brain
December 2012
Early Phase 1
AstraZeneca
Rheumatoid Arthritis
May 2009
Phase 1
GECEM
Arthritis, Rheumatoid
September 2015
Phase 3
Instituto de Cardiologia do Rio Grande do Sul
Heart Failure-Myocardial Ischemia
December 2007
Phase 2-Phase 3
CHA University
Ectopic Pregnancy
May 2013
Phase 3
Pakistan Institute of Learning and Living-Abbasi Shaheed Hospital-Dow University of Health Sciences-Karwan e Hayat, Karachi, Pakistan-Institute of Behavioural Sciences, Karachi, Pakistan
Schizophrenia-Schizoaffective Disorder-Schizophreniform Disorder
December 2013
Phase 1
Astellas Pharma Global Development, Inc.-Astellas Pharma Inc
Rheumatoid Arthritis
July 2016
Phase 1
Novartis
Rheumatoid Arthritis
March 2007
Phase 2
Nancy Samir Elbarbary-Ain Shams University
Acute Lymphoblastic Leukemia
June 2012
Phase 2
Postgraduate Institute of Medical Education and Research
Rheumatoid Arthritis
May 2011
Phase 4
Pfizer
Arthritis-Rheumatoid-High Dose
May 2011
Merck Sharp & Dohme Corp.-Integrated Therapeutics Group
Arthritis, Psoriatic
May 2006
Phase 3
Faculty of Medicine, University of Alexandria
Osteoarthritis
July 2011
Pfizer
Rheumatoid Arthritis
April 2005
Phase 1
Janssen-Cilag International NV
Psoriasis
October 2009
Phase 4
Nicklaus Children's Hospital f/k/a Miami Children's Hospital
Recurrent Childhood Medulloblastoma-Recurrent Childhood Ependymoma-Childhood Atypical Teratoid/Rhabdoid Tumor-Embryonal Tumor With Abundant Neuropil and True Rosettes-Metastatic Malignant Neoplasm to the Leptomeninges
February 2016
Phase 2
4SC AG
Rheumatoid Arthritis
November 2009
Phase 2
Janssen Research & Development, LLC
Arthritis, Juvenile
December 22, 2014
Phase 3
National Eye Institute (NEI)-National Institutes of Health Clinical Center (CC)
Non-infectious Intermediate and Posterior Uveitis
February 2011
Phase 1-Phase 2
Ege University
Ectopic Pregnancy-Infertility
January 2013
Polish Lymphoma Research Group
Lymphoma, T-Cell, Cutaneous-Mycosis Fungoides
June 2014
Phase 4
The University of Texas Health Science Center, Houston
Brain Tumor Recurrent
October 2016
Early Phase 1
Amgen-Immunex Corporation
Psoriasis
November 2009
Phase 3
Postgraduate Institute of Medical Education and Research
Psoriasis
August 2008
Phase 4
