colestilan colestilan colestilan (inn, trade name bindren) is a medication that acts as a phosphate binder and bile acid sequestrant. it is an ion-exchange resin, is an orally administered bile acid sequestrant that is being developed by mitsubishi tanabe pharma corporation for the treatment of hypercholesterolaemia and hyperphosphataemia. it has been launched in japan for hypercholesterolaemia. for the treatment of hyperphosphataemia, it is launched in austria, germany, the czech republic, portugal and the united kingdom, is registered in the eu. phase iii development in paediatric patients with hyperphosphataemia associated with chronic kidney disease was underway in the uk and germany. however, the company discontinued the development. in addition, the phase ii development in type-2 diabetes mellitus and phase i development in hyperphosphataemia, in japan, was also discontinued by the company. colestilanclinical datatrade namesbindrenahfs/drugs.cominternational drug namespregnancycategory b routes ofadministrationoralatc codev03ae06 (who) legal statuslegal status in general: ℞ (prescription only) pharmacokinetic databioavailabilitynot absorbedprotein bindingnametabolismnot absorbedexcretiongutidentifiers iupac name 2-(chloromethyl)oxirane 2-methyl-1h-imidazole copolymer cas number95522-45-5 ypubchem cid65840chemspidernoneuniivsi302rysrkeggd01934 ychemblchembl2103800 ncomptox dashboard (epa)dtxsid40914950 chemical and physical dataformula(c4h5cln2)m(c3h6o)n ny (what is this?) (verify) phase iii development for hyperphosphataemia was previously underway in the us. however, mitsubishi tanabe pharma discontinued development in this market. colestilan was also investigated in phase iii trials in europe and asia for hypercholesterolaemia. however, as of march 2015, no recent reports of development have been identified for the drug in this indication clinical use colestilan is used for the treatment of hyperphosphataemia (too high phosphate concentrations in the blood serum) in patients undergoing dialysis, including peritoneal dialysis. contraindications colestilan is contraindicated in patients with bowel obstruction. interactions the substance can inhibit the resorption of other drugs, as well as fat soluble vitamins (a, d, e, k) and folate, from the gut. resulting lower blood levels can be clinically problematic with immunosuppressant and antiepileptic drugs. adverse effects adverse effects include gastrointestinal problems such as constipation, as well as vitamin and calcium deficiency. vitamin k deficiency sometimes causes gastrointestinal bleeding. chemistry and mechanism of action colestilan is a cross-linked copolymer of 2-methylimidazole and epichlorohydrin and works as an anion exchanger resin with affinity to phosphate, bile acid anions and urate. it binds these anions in the gut and removes them from the enterohepatic circulation. colestilan is not absorbed from the gut, but is excreted together with the bound anions. 2-methyl-1h-imidazole (left) and epichlorohydrin (right) notes and references klement a (11 november 2013). "dialysepflichtig – weniger phosphat mit bindren". österreichische apothekerzeitung (in german) (23/2013): 28f. handelsman y (may 2011). "role of bile acid sequestrants in the treatment of type 2 diabetes". diabetes care. 34 suppl 2 (suppl 2): s244-50. doi:10.2337/dc11-s237. pmc 3632187. pmid 21525463. "drug profile:colestilan". adis insight. springer nature switzerland ag. december 2, 2015. retrieved december 16, 2015. haberfeld h, ed. (2013). austria-codex (in german). vienna: österreichischer apothekerverlag. bindren 1 g filmtabletten. drugs for treatment of hyperkalemia and hyperphosphatemia (v03ae)potassium binders patiromer polystyrene sulfonate sodium zirconium cyclosilicate phosphate binders aluminium hydroxide calcium acetate calcium acetate/magnesium carbonate calcium carbonate colestilan lanthanum carbonate sevelamer sucroferric oxyhydroxide lipid-modifying agents (c10)gi tractcholesterol absorption inhibitors, npc1l1 ezetimibe sch-48461 bile acid sequestrants/resins (ldl) colesevelam colestilan colestipol colestyramine colextran liverstatins (hmg-coa reductase, ldl) atorvastatin cerivastatin‡ fluvastatin lovastatin mevastatin pitavastatin pravastatin rosuvastatin simvastatin# niacin and derivatives (hdl and ldl) acipimox aluminium nicotinate niacin niceritrol nicofuranose nicotinyl alcohol mttp inhibitors (vldl) dirlotapide lomitapide mitratapide atp citrate lyase inhibitors (ldl) bempedoic acid blood vesselsfibrates (ppar) aluminium clofibrate bezafibrate choline fenofibrate ciprofibrate clinofibrate clofibrate‡ clofibride etofibrate fenofibrate gemfibrozil nafenopin pemafibrate ronifibrate simfibrate cetp inhibitors (hdl) anacetrapib† dalcetrapib§ evacetrapib§ obicetrapib† torcetrapib§ pcsk9 inhibitors (ldl) alirocumab bococizumab evolocumab combinations amlodipine/atorvastatin bempedoic acid/ezetimibe ezetimibe/atorvastatin ezetimibe/rosuvastatin ezetimibe/simvastatin fenofibrate/pravastatin fenofibrate/simvastatin niacin/laropiprant niacin/lovastatin niacin/simvastatin other alipogene tiparvovec azacosterol azalanstat benfluorex‡ darapladib§ dextrothyroxine‡ inclisiran lapaquistat§ magnesium pyridoxal 5-phosphate glutamate meglutol mipomersen omega-3-triglycerides policosanol probucol tiadenol triparanol‡ volanesorsen #who-em ‡withdrawn from market clinical trials: †phase iii §never to phase iii this article is issued from wikipedia. the text is licensed under creative commons - attribution - sharealike. additional terms may apply for the media files.