Investigational Drug Details
| Drug ID: | D283 |
| Drug Name: | Proanthocyanidin |
| Synonyms: | Crofelemer |
| Type: | Chemical drug |
| DrugBank ID: | DB04941 |
| DrugBank Description: | Crofelemer, previously known as the investigational drug SP-303, is a novel proanthocyanidin purified from the bark latex of the Amazonian Croton tree <i>Croton lechleri</i>. 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. |
| PubChem ID: | 108065 |
| CasNo: | 18206-61-6 |
| Repositioning for NAFLD: | Yes |
| SMILES: | O[C@@H]1[C@H](c2c(O[C@@H]1c1ccc(cc1)O)cc(cc2O)O)c1c2c(C[C@H]([C@H](O2)c2cc(O)c(c(c2)O)OC)O)c(cc1O)O |
| Structure: |
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| InChiKey: | JPFCOVZKLAXXOE-NFJBMHMQSA-N |
| Molecular Weight: | 592.553 |
| DrugBank Targets: | Cystic fibrosis transmembrane conductance regulator antagonist; Anoctamin-1 antagonist |
| DrugBank MoA: | Crofelemer is an inhibitor of the cystic fibrosis transmembrane regulator chloride channel (CFTR), as evidenced by its activity on cell cultures, single cell patch clamps, single CFTR channels, and elaboration of mouse intestinal fluid secretion. Crofelemer also inhibits calcium activated chloride channels (CaCC), which in combination with CFTR, are expressed on the luminal side of intestinal cells. Crofelemer inhibition of both of these channels prevents water loss from diarrhea by inhibiting chloride secretion. |
| DrugBank Pharmacology: | Crofelemer is an inhibitor of secretory diarrhea via inhibition of the CFTR chloride transporter. Crofelemer is not an antimicrobial, and therefore does not drive the emergence of resistance; it does not inhibit motility, and therefore does not cause constipation or rebound diarrhea; and it is not systemically absorbed, reducing the potential for adverse drug interactions and toxicity. |
| DrugBank Indication: | For the symptomatic treatment of non-infectious diarrhea in adult patients with HIV/AIDS who are taking antiretroviral therapy. |
| Targets: | CFTR antagonist |
| Therapeutic Category: | -- |
| Clinical Trial Progress: | Phase 2&3 on-going (ChiCTR-IPR-16008156) |
| Latest Progress: | Under clinical trials |
| Trial ID | Source ID | Phases | Status | Study Results | Start Date | Last Update Posted | |
|---|---|---|---|---|---|---|---|
| L0586 | ChiCTR-IPR-16008156 | Pilot study | Recruiting | No Results Available | 25/03/2016 | 18 April 2017 | Details |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S03 | Anti-fibrosis | fibrosis | Angiotensin Receptor Blocker (ARB); CCR2/CCR5 antagonist; Thyroid receptor β agonist; PEGylated human FGF21 analogue; Monoclonal antibody to lysyl oxidase-like 2 (LOXL2); Galectin-3 inhibitor; FGF19 variant | Losartan; Cenicriviroc; VK-2809; MGL-3196; Pegbelfermin; Simtuzumab; GR-MD-02; NGM282 | Details |
| Article ID | PMID | Source | Title | |
|---|---|---|---|---|
| A02927 | 34195217 | Front Nutr | Grape Polyphenols Attenuate Diet-Induced Obesity and Hepatic Steatosis in Mice in Association With Reduced Butyrate and Increased Markers of Intestinal Carbohydrate Oxidation. | Details |
| A06492 | 32856322 | J Pharm Pharmacol | Therapeutic effects of açaí seed extract on hepatic steatosis in high-fat diet-induced obesity in male mice: a comparative effect with rosuvastatin. | Details |
| A07253 | 32566176 | Food Sci Nutr | Lycium ruthenicum Murr. alleviates nonalcoholic fatty liver in mice. | Details |
| A11574 | 30833801 | World J Gastroenterol | Procyanidin B2 protects against diet-induced obesity and non-alcoholic fatty liver disease via the modulation of the gut microbiota in rabbits. | Details |
| A12789 | 30287733 | Nutrients | Achacha (Garcinia humilis) Rind Improves Cardiovascular Function in Rats with Diet-Induced Metabolic Syndrome. | Details |
| A13090 | 30142454 | Free Radic Biol Med | Procyanidin B2 ameliorates free fatty acids-induced hepatic steatosis through regulating TFEB-mediated lysosomal pathway and redox state. | Details |
| A14892 | 29189132 | Curr Pharm Des | Polyphenols: Novel Signaling Pathways. | Details |
| A20008 | 26207852 | J Agric Food Chem | Inhibition of Advanced Glycation Endproduct Formation by Lotus Seedpod Oligomeric Procyanidins through RAGE-MAPK Signaling and NF-κB Activation in High-Fat-Diet Rats. | Details |
| A22259 | 24712752 | J Med Food | Antioxidant properties of proanthocyanidins attenuate carbon tetrachloride (CCl4)-induced steatosis and liver injury in rats via CYP2E1 regulation. | Details |
| A22783 | 24307947 | J Lipids | Grape seed proanthocyanidin rescues rats from steatosis: a comparative and combination study with metformin. | Details |
| A25034 | 22227333 | Eur J Pharmacol | Flavangenol (pine bark extract) and its major component procyanidin B1 enhance fatty acid oxidation in fat-loaded models. | Details |
| A25233 | 22067945 | Lipids Health Dis | Polyphenolic extract of lotus root (edible rhizome of Nelumbo nucifera) alleviates hepatic steatosis in obese diabetic db/db mice. | Details |
| A46982 | 31336037 | Mol Nutr Food Res | The Preventative Effects of Procyanidin on Binge Ethanol-Induced Lipid Accumulation and ROS Overproduction via the Promotion of Hepatic Autophagy. | Details |
| A50627 | 35322435 | J Food Biochem | Chia seeds and chemical-elicited sprouts supplementation ameliorates insulin resistance, dyslipidemia, and hepatic steatosis in obese rats. | Details |
| A51877 | 33499382 | Nutrients | Rind from Purple Mangosteen (Garcinia mangostana) Attenuates Diet-Induced Physiological and Metabolic Changes in Obese Rats. | Details |
| A52264 | 29502000 | Environ Pollut | Dietary grape seed proanthocyanidin extract regulates metabolic disturbance in rat liver exposed to lead associated with PPARα signaling pathway. | Details |
| A52877 | 20332082 | Mol Cell Proteomics | Lipogenesis is decreased by grape seed proanthocyanidins according to liver proteomics of rats fed a high fat diet. | Details |