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Development Status

Investigational

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Primary Target

Integrin alpha-IIb/beta-3

2

Leukotriene B4 receptor 1

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Highest Phase

Phase II

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Approval Year

Unknown

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Condition

Myocardial infarction

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Unstable angina

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Asthma

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Chronic obstructive pulmonary disease

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Cystic fibrosis

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Treatment Modality

Primary

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Originator

Dr. Karl Thomae

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Boehringer Ingelheim

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Substance Class

Chemical

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Code System

CAS

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ChEMBL

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DRUG BANK

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EPA CompTox

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FDA UNII

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Substance Form

Principal Form

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Salts, Hydrates, Esters, etc.

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Showing 1 - 3 of 3 results

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AMELUBANT

E0018IF0K4

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Leukotriene B4 receptor 1

Conditions:

Rheumatoid arthritis

Chronic obstructive pulmonary disease

Cystic fibrosis

Amelubant, its metabolite BIIL 260 (formed by removal of the ethoxycarbonyl protecting group), and its major metabolite BIIL 315 (formed by removal of the protecting group and glucuronidation) had potent in vitro and in vivo Leukotriene B4 receptor a...

ntagonistic properties. Amelubant has been in phase II clinical trials by Boehringer Ingelheim for the treatment of cystic fibrosis, chronic obstructive pulmonay disease, bronchial asthma and rheumatoid arthritis. However, this research has been discontinued. In 2002, orphan drug designation was received in E.U. for the treatment of cystic fibrosis. Serious adverse events of Amelubant were characterized by increased presentation of respiratory signs and/or symptoms associated with pulmonary exacerbation and resulted in admission to a hospital and/or administration of IV antibiotics.

FRADAFIBAN

DQ0H2B8YKN

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Integrin alpha-IIb/beta-3

Integrin alpha-IIb/beta-3

Conditions:

Myocardial infarction

Unstable angina

Lefradafiban, an orally active prodrug of fradafiban, is a novel glycoprotein (IIb/IIIa) inhibitor for the treatment of unstable angina. The pharmacokinetic and pharmacodynamic properties of lefradafiban were assessed in 130 healthy male volunteers ...

who received a single dose of 10, 50, 75, 100, or 150 mg or multiple doses of 25, 50, 60, 75, 90, or 100 mg three times daily for one week. After both single and multiple doses, receptor occupancy and plasma lefradafiban levels correlated with platelet aggregation. Lefradafiban had been in phase II clinical trials by Boehringer Ingelheim for the treatment of thrombosis. However, it has been terminated.

LEFRADAFIBAN

0R4888YXR5

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Integrin alpha-IIb/beta-3

Integrin alpha-IIb/beta-3

Conditions:

Myocardial infarction

Unstable angina

Lefradafiban, an orally active prodrug of fradafiban, is a novel glycoprotein (IIb/IIIa) inhibitor for the treatment of unstable angina. The pharmacokinetic and pharmacodynamic properties of lefradafiban were assessed in 130 healthy male volunteers ...

who received a single dose of 10, 50, 75, 100, or 150 mg or multiple doses of 25, 50, 60, 75, 90, or 100 mg three times daily for one week. After both single and multiple doses, receptor occupancy and plasma lefradafiban levels correlated with platelet aggregation. Lefradafiban had been in phase II clinical trials by Boehringer Ingelheim for the treatment of thrombosis. However, it has been terminated.

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