Delving into the Latest Updates on Colestilan with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

BindRen, COLESTILAN CHLORIDE, Colestimide

+ [5]

Target

Phosphates

Mechanism

Phosphates modulators(Phosphates modulators)

Therapeutic Areas

Endocrinology and Metabolic Disease

Active Indication

Heterozygous familial hypercholesterolemiaHypercholesterolemia

Inactive Indication

Chronic kidney disease, Stage VChronic Kidney DiseasesDiabetes Mellitus, Type 2+ [1]

Originator Organization

Mitsubishi Tanabe Pharma Factory Ltd.

Active Organization

Fuji Pharma Co., Ltd.Mitsubishi Tanabe Pharma Factory Ltd.

Inactive Organization

Mitsubishi Tanabe Pharma Corp.Mitsubishi Tanabe Pharma Europe Ltd.

Drug Highest PhaseApproved

First Approval Date

JP (12 Mar 1999),

Heterozygous familial hypercholesterolemiaHypercholesterolemia

Regulation-

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Structure

Molecular FormulaC7H11ClN2O

InChIKeyDEMLYXMVPJAVFU-UHFFFAOYSA-N

CAS Registry95522-45-5

A Multi-centre, Randomised, Controlled, Parallel Group, Open-label Study Evaluating the Efficacy, Safety and Tolerability of Three Doses of Colestilan (MCI-196) Compared to Standard Therapy With a Calcium-based Phosphate Binder, in Paediatric Subjects With Chronic Kidney Disease Stage 5 on Dialysis and With Hyperphosphataemia

The Primary Objective of this study is to determine the initial starting doses of colestilan (MCI-196) in paediatric subjects with Chronic Kidney Disease Stage 5 on Dialysis and with Hyperphosphataemia.

Start Date01 Apr 2014

Sponsor / Collaborator

Mitsubishi Tanabe Pharma Corp.

NCT01976572 / CompletedPhase 1

A Randomised, Open-Label, Drug-Drug Interaction Study to Evaluate the Effect of Colestilan on the Pharmacokinetics of Single Oral Doses of Candesartan Cilexetil in Healthy Subjects

The primary objective is to assess the effects of colestilan on the pharmacokinetic profile of candesartan cilexetil when administered at the same time as, 1 hour before, and 3 hours after the first daily dose of colestilan administered at doses of 5 g three times daily compared to administration of candesartan cilexetil alone, in healthy subjects.

Start Date01 Oct 2013

Sponsor / Collaborator

Mitsubishi Tanabe Pharma Corp.

100 Clinical Results associated with Colestilan

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100 Translational Medicine associated with Colestilan

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100 Patents (Medical) associated with Colestilan

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88

Literatures (Medical) associated with Colestilan

19 Jun 2023·Gels (Basel, Switzerland)

Bile Acid Sequestrants Based on Natural and Synthetic Gels.

Review

Author: Stanciu, Magdalena-Cristina ; Nichifor, Marieta ; Teacă, Carmen-Alice

Bile acid sequestrants (BASs) are non-systemic therapeutic agents used for the management of hypercholesterolemia. They are generally safe and not associated with serious systemic adverse effects. Usually, BASs are cationic polymeric gels that have the ability to bind bile salts in the small intestine and eliminate them by excretion of the non-absorbable polymer-bile salt complex. This review gives a general presentation of bile acids and the characteristics and mechanisms of action of BASs. The chemical structures and methods of synthesis are shown for commercial BASs of first- (cholestyramine, colextran, and colestipol) and second-generation (colesevelam and colestilan) and potential BASs. The latter are based on either synthetic polymers such as poly((meth)acrylates/acrylamides), poly(alkylamines), poly(allylamines) and vinyl benzyl amino polymers or biopolymers, such as cellulose, dextran, pullulan, methylan, and poly(cyclodextrins). A separate section is dedicated to molecular imprinting polymers (MIPs) because of their great selectivity and affinity for the template molecules used in the imprinting technique. Focus is given to the understanding of the relationships between the chemical structure of these cross-linked polymers and their potential to bind bile salts. The synthetic pathways used in obtaining BASs and their in vitro and in vivo hypolipidemic activities are also introduced.

01 Aug 2022·JGH Open

Usefulness of colestimide for diarrhea in postoperative Crohn's disease

Article

Author: Morikubo, Hiromu ; Miyatani, Yusuke ; Matsuda, Takahisa ; Hibi, Toshifumi ; Fukuda, Tomohiro ; Hojo, Aya ; Nakano, Masaru ; Sagami, Shintaro ; Matsubayashi, Mao ; Kobayashi, Taku ; Asonuma, Kunio

AbstractBackground and AimCrohn's disease (CD) often causes intractable diarrhea after intestinal resection. Anion exchange resins have been reported to be effective in patients with bile acid diarrhea after distal ileectomy; furthermore, bile acid metabolism has been implicated in the pathogenesis of CD. Therefore, we aimed to examine the effectiveness of colestimide in the management of postoperative CD, and to compare its impact between patients with and those without ileocecal resection.MethodsPostoperative CD patients prescribed colestimide for diarrhea between April 2017 and December 2020 were retrospectively evaluated for changes in the total Crohn's disease activity index (CDAI), each CDAI component including diarrhea frequency/week, albumin, and C‐reactive protein (CRP) was evaluated before and after the administration of colestimide. Furthermore, comprehensive patient and physician assessments were reviewed from medical records during the first outpatient visit as a global clinical judgment after the initiation of colestimide therapy.ResultsA total of 24 patients were included, of whom 17 had a previous history of ileocecal resection. Significant improvement was noted in CDAI and diarrhea frequency only in the ileocecal resection group (CDAI: 114.5 ± 52.7 and 95.4 ± 34.8, P < 0.05; diarrhea frequency/week 23.8 ± 14.1 and 15.4 ± 11.2, P < 0.05, respectively). There was no significant improvement in other CDAI components, albumin level, or CRP level in either group. In the global clinical judgment, 13 and 4 patients in the ileocecal and non‐ileocecal resection groups, respectively, were judged as “effective,” with an overall efficacy rate of 70.8%.ConclusionColestimide is effective for diarrhea in patients with postoperative CD, especially after ileocecal resection.

01 May 2022·Clinica Chimica ActaQ3 · MEDICINE

Clinical and genetic features of sitosterolemia in Japan

Q3 · MEDICINE

Article

Author: Kojima, Nobuko ; Yamagami, Kan ; Kawashiri, Masa-Aki ; Takamura, Masayuki ; Tada, Hayato

BACKGROUND AND AIMClinical manifestations and genetic backgrounds of Japanese patients with sitosterolemia have been unclear.MATERIALS AND METHODSWe searched PubMed for studies using the keywords "sitosterolemia" or "phytosterolemia" and "Japan". Moreover, we added information from the members of the Committee on Primary Dyslipidemia under the Research Program on Rare and Intractable Disease of the Ministry of Health, Labour and Welfare (MHLW) of Japan.RESULTSWe identified 36 patients with sitosterolemia caused by biallelic pathogenic mutations in the ATP-binding cassette subfamily G member 5 (ABCG5) or ATP-binding cassette subfamily G member 8 (ABCG8) from 31 families in Japan. The diagnosed age ranged from 0 to 64 years (median 13 years). The median sitosterol and LDL cholesterol levels were 100 μg/ml (IQR: 50-183), and 193 mg/dl (IQR: 108-295), respectively. All the patients exhibited cutaneous and/or tendon xanthomas, up to 9 (25%) patients exhibited premature coronary artery disease, 5 (16%) patients exhibited arthritis, and 8 (22%) patients exhibited blood abnormalities. Ezetimibe was administered to all the patients, including infantile cases, while statins, colestimide, evolocumab, probucol, and LDL apheresis were also used.CONCLUSIONWe are providing a demographic overview of the clinical and genetic backgrounds of Japanese patients with sitosterolemia.

100 Deals associated with Colestilan

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Colestilan	V03AE06	DB11634

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Heterozygous familial hypercholesterolemia	JP	Mitsubishi Tanabe Pharma Factory Ltd.	12 Mar 1999
Heterozygous familial hypercholesterolemia	JP	Fuji Pharma Co., Ltd.	12 Mar 1999
Hypercholesterolemia	JP	Mitsubishi Tanabe Pharma Factory Ltd.	12 Mar 1999
Hypercholesterolemia	JP	Fuji Pharma Co., Ltd.	12 Mar 1999

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Hyperphosphatemia	Phase 2	NO	Mitsubishi Tanabe Pharma Europe Ltd.	21 Jan 2013
Hyperphosphatemia	Phase 2	EU	Mitsubishi Tanabe Pharma Europe Ltd.	21 Jan 2013
Hyperphosphatemia	Phase 2	LI	Mitsubishi Tanabe Pharma Europe Ltd.	21 Jan 2013
Hyperphosphatemia	Phase 2	LI	Mitsubishi Tanabe Pharma Europe Ltd.	21 Jan 2013
Hyperphosphatemia	Phase 2	EU	Mitsubishi Tanabe Pharma Europe Ltd.	21 Jan 2013
Hyperphosphatemia	Phase 2	NO	Mitsubishi Tanabe Pharma Europe Ltd.	21 Jan 2013
Hyperphosphatemia	Preclinical	IS	Mitsubishi Tanabe Pharma Europe Ltd.	21 Jan 2013

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00772382 (Pubmed \| Blood Purif) Manual	Phase 3	Hyperphosphatemia \| Chronic Kidney Diseases	116	Colestilan	(tqenyvpkdk) = mfpfoqgbzy lgcskzgeao (lrvfaeswvm )	Positive	01 Jan 2016
NCT00506441 (Pubmed \| Nephron)	Phase 3	Complication of renal dialysis \| Chronic Kidney Diseases	245	Colestilan	wilihxcmar(hkefynmepz) = oghmronagx ktkibsawhx (zzzrcbopux )	Positive	01 Jan 2015
NCT00858637 (CTgov)	Phase 3	Dyslipidemias \| Chronic Kidney Diseases	260	Simvastin+Placebo+MCI-196 (MCI-196 (Active) + Simvastin (Placebo)/ Withdrawal Phase)	hbhtxoalai(qdczjaeomy) = kvbckjknxr frtbrqdgum (wfdsupbgka, txktqzijhu - swekwhfugk)	-	17 Oct 2014
				Simvastin+Placebo+MCI-196 (MCI-196 (Placebo) + Simvastin (Placebo)/ Withdrawal Phase)	hbhtxoalai(qdczjaeomy) = vvbcynidkc frtbrqdgum (wfdsupbgka, kuktydxpmn - xbfdbqxmmh)
NCT00542386 (CTgov)	Phase 3	Hyperphosphatemia \| Chronic kidney disease, Stage V \| Dyslipidemias	642	MCI-196 (MCI-196: 3 g)	ltvkmrkosy(nxjfbwmknd) = ymaftasbeo gbsiupjcyu (cjdpsojuyt, voeyjrzgjw - rierdbbebt) View more	-	06 Oct 2014
				MCI-196 (MCI-196: 6 g)	ltvkmrkosy(nxjfbwmknd) = zgktpftubn gbsiupjcyu (cjdpsojuyt, sppzquncms - mtroovbfne) View more
NCT00772382 (CTgov)	Phase 3	Hyperphosphatemia \| Chronic kidney disease, Stage V	116	MCI-196	lsunohnvql(watdmqbdju) = qxnjgzybfl cxhfgbyghq (ldpwlsufcq, cndyghoxjy - vnintjikjc) View more	-	12 May 2014
MP215 (ERA2014)	Phase 2/3	Hyperphosphatemia	-	Colestilan alone	glxgvmnbbd(dchbgwvhhh) = margdvlfym kfvguwxofo (dvliqnvymd ) View more	Positive	01 May 2014
				Colestilan plus calcium phosphate binder	(ovhmzzgkgp) = ygwwlvtrms ehlctwnqsu (jsizhxjwtx ) View more
ASN2011	Not Applicable	Hyperphosphatemia \| Dyslipidemias \| Chronic Kidney Diseases HbA1c \| uric acid	642	Colestilan 3g/day	ijqurxmssx(uyoqkoafya) = jftlppspvp xsevzjfcxi (ipbqcyyjhq )	Positive	08 Nov 2011
				Colestilan 6g/day	ijqurxmssx(uyoqkoafya) = lkcwticpzt xsevzjfcxi (ipbqcyyjhq )
NCT00497198 (CTgov)	Phase 2	Diabetes Mellitus, Type 2	183	MCI-196 (MCI-196)	twcuqwqlvb(mbgvicjdhz) = hiexnyfaih gqelkdqbgb (rohlyqibnv, czabhqdtuu - bjwxccueat) View more	-	11 Aug 2011
				Placebo of MCI-196 Tablet (Placebo)	twcuqwqlvb(mbgvicjdhz) = nmcayuavfo gqelkdqbgb (rohlyqibnv, mpweyqypct - gjhskmhnxi) View more