DescriptionCurator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/19808995
http://broom02.revolvy.com/main/index.php?s=Crofelemer&item_type=topic; http://www.hivandhepatitis.com/hiv-aids/hiv-aids-topics/hiv-related-conditions/3928-fda-approves-diarrhea-drug-crofelemer-for-people-with-hivaids
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/19808995
http://broom02.revolvy.com/main/index.php?s=Crofelemer&item_type=topic; http://www.hivandhepatitis.com/hiv-aids/hiv-aids-topics/hiv-related-conditions/3928-fda-approves-diarrhea-drug-crofelemer-for-people-with-hivaids
Crofelemer, previously known as the investigational drug SP-303, is a novel proanthocyanidin purified from the bark latex of the Amazonian Croton tree Croton lechleri. It is marketed under the brand name Fulyzaq and indicated for the symptomatic treatment of non-infectious diarrhea in adult patients with HIV/AIDS who are taking antiretroviral therapy. Fulyzaq treats the symptoms of disease, but it is not used to treat infectious diarrhea (diarrhea caused by infection of the digestive system by a bacteria, virus or parasite). It was initially developed by Napo Pharmaceuticals, which licensed it to Glenmark Pharmaceuticals in 140 emerging markets and to Salix Pharmaceuticals in the US, EU and some other markets. A Phase III clinical trial for diarrhoea in HIV patients was completed in 2012, and the drug was approved by the US Food and Drug Administration (FDA) on 31 December 2012.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P13569 Gene ID: 1080.0 Gene Symbol: CFTR Target Organism: Homo sapiens (Human) |
7.0 µM [IC50] | ||
Target ID: Q5XXA6 Gene ID: 55107.0 Gene Symbol: ANO1 Target Organism: Homo sapiens (Human) |
6.5 µM [IC50] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Secondary | FULYZAQ Approved UseAn anti-diarrheal indicated for the symptomatic relief of non-infectious diarrhea in adult patients with HIV/AIDS on anti-retroviral therapy Launch Date2012 |
PubMed
Title | Date | PubMed |
---|---|---|
Crofelemer, an antisecretory antidiarrheal proanthocyanidin oligomer extracted from Croton lechleri, targets two distinct intestinal chloride channels. | 2010 Jan |
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Crofelemer (Fulyzaq) for antiretroviral-induced diarrhea. | 2013 Jul 22 |
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Efficacy and safety of crofelemer for noninfectious diarrhea in HIV-seropositive individuals (ADVENT trial): a randomized, double-blind, placebo-controlled, two-stage study. | 2013 Nov-Dec |
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Crofelemer: In HIV Associated Diarrhea and Secretory Diarrhea - A Patent Perspective. | 2014 |
Sample Use Guides
The recommended dose of FULYZAQ (crofelemer) is one 125 mg delayed-release tablettaken orally two 7 times a day, with or without food.
Route of Administration:
Oral
In Vitro Use Guide
Sources: http://www.ncbi.nlm.nih.gov/pubmed/?term=19808995
In Cyclic Nucleotide Assays T84 cells were grown in 24-well plates, treated for 45 min with crofelemer 50 uM crofelemer and then for 10 min with 0 or 20 μM forskolin, lysed by sonication, and centrifuged to remove cell debris, and the supernatant was assayed for cAMP according to manufacturer's instructions (Parameter cAMP immunoassay kit; R&D Systems, Minneapolis, MN).
Substance Class |
Polymer
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LIVERTOX |
NBK548325
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FDA ORPHAN DRUG |
897722
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NCI_THESAURUS |
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FDA ORPHAN DRUG |
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