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Description
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.

Originator

Curator's Comment: Crofelemer was discovered by Napo Pharmaceuticals and developed jointly with Salix Pharmaceuticals

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
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

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
FULYZAQ

Approved Use

An anti-diarrheal indicated for the symptomatic relief of non-infectious diarrhea in adult patients with HIV/AIDS on anti-retroviral therapy

Launch Date

2012
PubMed

PubMed

TitleDatePubMed
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 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).
Name Type Language
CROFELEMER
DASH   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN  
Official Name English
SP-303
Code English
CROFELEMER [MI]
Common Name English
TRN-002
Code English
MYTESI
Brand Name English
CROFELEMER [ORANGE BOOK]
Common Name English
CROFELEMER [USAN]
Common Name English
NP-303
Code English
Crofelemer [WHO-DD]
Common Name English
CROFELEMER [VANDF]
Common Name English
FULYZAQ
Brand Name English
VIREND
Brand Name English
PROVIR
Brand Name English
Classification Tree Code System Code
LIVERTOX NBK548325
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NDF-RT N0000178374
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WHO-ATC A07XA06
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FDA ORPHAN DRUG 897722
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NCI_THESAURUS C266
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FDA ORPHAN DRUG 592017
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Code System Code Type Description
MERCK INDEX
m11702
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PRIMARY
WIKIPEDIA
CROFELEMER
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PRIMARY
DAILYMED
PY79D6C8RX
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PRIMARY
MESH
C546704
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EPA CompTox
DTXSID50858715
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FDA UNII
PY79D6C8RX
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RXCUI
1364449
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PRIMARY RxNorm
USAN
KK-02
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PRIMARY
IUPHAR
7453
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PRIMARY
ChEMBL
CHEMBL2108184
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DRUG CENTRAL
4744
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DRUG BANK
DB04941
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PRIMARY
CAS
148465-45-6
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PRIMARY
NCI_THESAURUS
C125392
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Display Structure of CROFELEMER