BIXALOMER

Description
Sources: https://www.astellas.com/en/corporate/news/pdf/120625_Eg.pdf | https://www.ncbi.nlm.nih.gov/pubmed/28194884

Bixalomer (development code: ASP15 and brand name Kiklin) is a metal-free, nonabsorbable is approved in Japan to treat hyperphosphatemia in dialysis patients. Hyperphosphatemia occurs in patients whose renal function is decreased, since phosphorus is not sufficiently excreted into urine via the kidneys and consequently accumulates in the body. Bixalomer is amine-functional polymers which decrease the serum phosphorus concentration by binding to phosphate in the gastrointestinal tract, thus inhibiting absorption of phosphate into the human body.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
phosphate 1 Target ID: phosphate Sources: https://www.ncbi.nlm.nih.gov/pubmed/26452517	Binding Agent 1076

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hyperphosphatemia 30 Sources: https://www.astellas.com/en/corporate/news/pdf/120625_Eg.pdf	Primary		Approved 8583	Kiklin Approved Use for the indication of treatment of hyperphosphatemia in patients with chronic kidney disease Launch Date 2012

C_max

Value	Dose	Co-administered	Analyte	Population
0 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/800126_2190032M1027_1_018_1F.pdf#page=36	2500 mg single, oral dose: 2500 mg route of administration: Oral experiment type: SINGLE co-administered:		BIXALOMER plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

AUC

Value	Dose	Co-administered	Analyte	Population
0 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/800126_2190032M1027_1_018_1F.pdf#page=36	2500 mg single, oral dose: 2500 mg route of administration: Oral experiment type: SINGLE co-administered:		BIXALOMER plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FED

Doses

Dose	Population	Adverse events
7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/	Disc. AE: Constipation, Gastroesophagitis... AEs leading to discontinuation/dose reduction: Constipation (1.25%) Gastroesophagitis (1.25%) Upper gastrointestinal hemorrhage (1.25%) Vomiting (1.25%) Chest discomfort (1.25%) Hyponatremia (1.25%) Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/
7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581	Disc. AE: Intestinal obstruction, Intestinal perforation... AEs leading to discontinuation/dose reduction: Intestinal obstruction Intestinal perforation Ischemic enterocolitis Gastrointestinal bleeding Gastrointestinal ulcer Constipation Diverticulitis Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581
7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24720402/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/24720402/	Sources: https://pubmed.ncbi.nlm.nih.gov/24720402/

AEs

AE	Significance	Dose	Population
Chest discomfort	1.25% Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/
Constipation	1.25% Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/
Gastroesophagitis	1.25% Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/
Hyponatremia	1.25% Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/
Upper gastrointestinal hemorrhage	1.25% Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/
Vomiting	1.25% Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/27896908/
Constipation	Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581
Diverticulitis	Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581
Gastrointestinal bleeding	Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581
Gastrointestinal ulcer	Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581
Intestinal obstruction	Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581
Intestinal perforation	Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581
Ischemic enterocolitis	Disc. AE	7.5 g 1 times / day multiple, oral Recommended Dose: 7.5 g, 1 times / day Route: oral Route: multiple Dose: 7.5 g, 1 times / day Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.rad-ar.or.jp/siori/english/kekka_plain.cgi?n=32581

PubMed

Title	Date	PubMed
Long-Term Safety and Efficacy of Bixalomer in Hyperphosphatemic Patients With Chronic Kidney Disease Not on Dialysis.	2017-04	28194884
Research on kidney and mineral metabolism in Japan: past, present, and future.	2017-03	28005175
Bixalomer in Hyperphosphatemic Patients With Chronic Kidney Disease Not on Dialysis: Phase 3 Randomized Trial.	2016-12	27896908
Bixalomer, a novel phosphate binder with a small swelling index, improves hyperphosphatemia in chronic kidney disease rat.	2015-11-05	26452517

Sample Use Guides

In Vivo Use Guide

Kiklin (bixalomer) is usually taken orally 2 capsules, 3 times per day or as directed by a doctor. The capsules should be taken just before meals along with some water.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Name

Type

Language

KIKLIN

Preferred Name

English

BIXALOMER

Official Name

English

AMG-223

Code

English

Bixalomer [WHO-DD]

Common Name

English

ASP1585

Code

English

BIXALOMER [USAN]

Common Name

English

ILY101

Code

English

ILY-101

Code

English

1,4-BUTANEDIAMINE, N,N,N',N'-TETRAKIS(3-AMINOPROPYL)-, POLYMER WITH 2-(CHLOROMETHYL)OXIRANE

Common Name

English

BIXALOMER [JAN]

Common Name

English

ASP-1585

Code

English

N,N,N',N'-TETRAKIS(3-AMINOPROPYL)BUTANE-1,4-DIAMINE POLYMER WITH 2-(CHLOROMETHYL)OXIRANE

Common Name

English

BIXALOMER [MI]

Common Name

English

bixalomer [INN]

Common Name

English

Code System Code Type Description

INN

9096