# Colestilan

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Chemical compound

Pharmaceutical compound

Colestilan Clinical data Trade names BindRen AHFS/Drugs.com International Drug Names Pregnancy category B Routes of administration Oral ATC code V03AE06 (WHO) Legal status Legal status In general: ℞ (Prescription only) Pharmacokinetic data Bioavailability Not absorbed Protein binding NA Metabolism Not absorbed Excretion Gut Identifiers IUPAC name 2-(chloromethyl)oxirane 2-methyl-1H-imidazole copolymer CAS Number 95522-45-5 Y PubChem CID 65840 ChemSpider none UNII VSI302RYSR KEGG D01934 Y ChEMBL ChEMBL2103800 N CompTox Dashboard (EPA) DTXSID40914950 Chemical and physical data Formula (C4H5ClN2)m(C3H6O)n NY (what is this?) (verify)

**Colestilan** ([INN](/source/International_Nonproprietary_Name), trade name **BindRen**) is a [medication](/source/Medication) that acts as a [phosphate binder](/source/Phosphate_binder)[1] and [bile acid sequestrant](/source/Bile_acid_sequestrant).[2] 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.[3]

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[3]

## Clinical use

Colestilan is used for the treatment of [hyperphosphataemia](/source/Hyperphosphataemia) (too high [phosphate](/source/Phosphate) concentrations in the blood serum) in patients undergoing [dialysis](/source/Kidney_dialysis), including [peritoneal dialysis](/source/Peritoneal_dialysis).[1][4]

## Contraindications

Colestilan is contraindicated in patients with bowel obstruction.[4]

## Interactions

The substance can inhibit the resorption of other drugs, as well as fat soluble vitamins ([A](/source/Vitamin_A), [D](/source/Vitamin_A), [E](/source/Vitamin_A), [K](/source/Vitamin_A)) and [folate](/source/Folate), from the gut.[1] Resulting lower blood levels can be clinically problematic with [immunosuppressant](/source/Immunosuppressant) and [antiepileptic](/source/Antiepileptic) drugs.[4]

## Adverse effects

Adverse effects include [gastrointestinal problems](/source/Gastrointestinal_problem) such as constipation, as well as vitamin and [calcium](/source/Calcium) deficiency. Vitamin K deficiency sometimes causes gastrointestinal bleeding.[1][4]

## Chemistry and mechanism of action

Colestilan is a cross-linked [copolymer](/source/Copolymer) of [2-methylimidazole](/source/2-Methylimidazole) and [epichlorohydrin](/source/Epichlorohydrin) and works as an [anion exchanger](/source/Anion_exchanger) resin with affinity to [phosphate](/source/Phosphate), [bile acid](/source/Bile_acid) anions and [urate](/source/Urate). It binds these anions in the gut and removes them from the [enterohepatic circulation](/source/Enterohepatic_circulation). Colestilan is not absorbed from the gut, but is excreted together with the bound anions.[1]

2-methyl-1*H*-imidazole (left) and epichlorohydrin (right)

## Notes and references

1. ^ [***a***](#cite_ref-Klement_1-0) [***b***](#cite_ref-Klement_1-1) [***c***](#cite_ref-Klement_1-2) [***d***](#cite_ref-Klement_1-3) [***e***](#cite_ref-Klement_1-4) Klement A (11 November 2013). "Dialysepflichtig – weniger Phosphat mit BindRen". *Österreichische Apothekerzeitung* (in German) (23/2013): 28f.

1. **[^](#cite_ref-2)** Handelsman Y (May 2011). ["Role of bile acid sequestrants in the treatment of type 2 diabetes"](https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3632187). *Diabetes Care*. 34 Suppl 2 (Suppl 2): S244-50. [doi](/source/Doi_(identifier)):[10.2337/dc11-s237](https://doi.org/10.2337%2Fdc11-s237). [PMC](/source/PMC_(identifier)) [3632187](https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3632187). [PMID](/source/PMID_(identifier)) [21525463](https://pubmed.ncbi.nlm.nih.gov/21525463).

1. ^ [***a***](#cite_ref-Spring_3-0) [***b***](#cite_ref-Spring_3-1) ["Drug Profile:Colestilan"](http://adisinsight.springer.com/drugs/800001537). *Adis Insight*. Springer Nature Switzerland AG. December 2, 2015. Retrieved December 16, 2015.

1. ^ [***a***](#cite_ref-AustriaCodex_4-0) [***b***](#cite_ref-AustriaCodex_4-1) [***c***](#cite_ref-AustriaCodex_4-2) [***d***](#cite_ref-AustriaCodex_4-3) Haberfeld H, ed. (2013). *Austria-Codex* (in German). Vienna: Österreichischer Apothekerverlag. BindRen 1 g Filmtabletten.

v t e 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

v t e Lipid-lowering agents (C10) GI tract Cholesterol absorption inhibitors, NPC1L1 Ezetimibe Hyzetimibe SCH-48461 Bile acid sequestrants/resins (LDL) Colesevelam Colestilan Colestipol Colestyramine Colextran Soluble fiber such as psyllium and glucomannan Liver Statins (HMG-CoA reductase, LDL) Atorvastatin Cerivastatin‡ Fluvastatin Lovastatin Mevastatin Pitavastatin Pravastatin Rosuvastatin Simvastatin# Niacin and derivatives (HDL and LDL) Acipimox Aluminium nicotinate Nicotinic acid Niceritrol Nicofuranose Nicotinyl alcohol MTTP inhibitors (VLDL) Dirlotapide Lomitapide Mitratapide ATP citrate synthase inhibitors (LDL) Bempedoic acid Thyromimetics (VLDL) Dextrothyroxine‡ Resmetirom Blood vessels PPAR agonists (LDL) Fibrates Aluminium clofibrate Bezafibrate Choline fenofibrate Ciprofibrate Clinofibrate Clofibrate‡ Clofibride Etofibrate Fenofibrate Gemfibrozil Nafenopin Pemafibrate Ronifibrate Simfibrate Others GW501516§ CETP inhibitors (HDL) Anacetrapib† Dalcetrapib§ Evacetrapib§ Obicetrapib† Torcetrapib§ PCSK9 inhibitors (LDL) Alirocumab Bococizumab Enlicitide† Evolocumab Inclisiran Lerodalcibep ANGPTL3 inhibitors (LDL/HDL) Evinacumab 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§ Lapaquistat§ Magnesium pyridoxal 5-phosphate glutamate Meglutol Mipomersen Olezarsen Omega−3-acid ethyl esters Plozasiran Policosanol Probucol Tiadenol Triparanol‡ Volanesorsen #WHO-EM ‡Withdrawn from market Clinical trials: †Phase III §Never to phase III

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Adapted from the Wikipedia article [Colestilan](https://en.wikipedia.org/wiki/Colestilan) by Wikipedia contributors ([contributor history](https://en.wikipedia.org/wiki/Colestilan?action=history)). Available under [Creative Commons Attribution-ShareAlike 4.0 International](https://creativecommons.org/licenses/by-sa/4.0/). Changes may have been made.