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Protein-arginine N-methyltransferase 1

8

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

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Investigational

6

Other

2

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Phase III

3

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Approval Year

Unknown

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Condition

African trypanosomiasis

3

Malaria

3

Pneumocystis pneumonia

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Treatment Modality

Curative

3

Preventing

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CNS Activity

CNS Penetrant

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Originator

University of North Carolina|Georgia State University|Auburn University|Duke University

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Chemical

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PUBCHEM

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EPA CompTox

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Showing 1 - 8 of 8 results

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FURAMIDINE

08GH1YF0RA

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

NADH-cytochrome b5 reductase

Cytochrome P450 4F2

Docosahexaenoic acid omega-hydroxylase CYP4F3

Protein-arginine N-methyltransferase 1

Quinone reductase 2

Conditions:

Pneumocystis pneumonia

African trypanosomiasis

Pafuramidine or DB289, [2,5-bis-(4-amidinophenyl)furan bis-O-methylamidoxime] is a pro-drug of DB75, [2,5-bis(4-amidinophenyl)furan] also known as furamidine. The biotransformation process of DB289 to DB75 in the human liver consists of three O-demet...

hylation reactions catalyzed by the Cyp4F enzyme subfamily and three N-dehydroxylation reactions catalyzed by cytrochrome b5 and NADH-cytochrome b5 reductase. DB289 was studied for therapeutic treatment against human African trypanosomiasis, Pneumocystis pneumonia and malaria. In November 2006, Immtech Pharmaceuticals, Inc. announced that the U.S. Food and Drug Administration (FDA) had granted orphan drug designation for pafuramidine (DB289) to treat Pneumocystis jiroveci pneumonia (PCP), a common life-threatening opportunistic infection in HIV/AIDS and other immunosuppressed patients. Despite the high efficacy of DB289 in patients, the mechanism of action of DB75 is unknown. The mechanism of antimicrobial activity of diamidine compounds is incompletely understood. They undergo active uptake by purine transporter systems in trypanosomes and their mechanism of action may involve interference with DNA-associated enzymes inhibition of heme crystallization11 or/and collapse of the transmitochondrial membrane potential.

PUTRESCINE

V10TVZ52E4

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Protein-arginine N-methyltransferase 1

Ornithine decarboxylase

J Urea Acid

2QJN9485J7

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Protein-arginine N-methyltransferase 1

Sulfone, bis((4-chloroacetylamino)phenyl)

JW87Q22JDK

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Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Protein-arginine N-methyltransferase 1

1,4-BUTANEDIAMINE ADIPATE

8N4WWW5620

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Protein-arginine N-methyltransferase 1

Ornithine decarboxylase

PAFURAMIDINE

H1VG379J2X

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

NADH-cytochrome b5 reductase

Cytochrome P450 4F2

Docosahexaenoic acid omega-hydroxylase CYP4F3

Protein-arginine N-methyltransferase 1

Quinone reductase 2

Conditions:

Pneumocystis pneumonia

African trypanosomiasis

Pafuramidine or DB289, [2,5-bis-(4-amidinophenyl)furan bis-O-methylamidoxime] is a pro-drug of DB75, [2,5-bis(4-amidinophenyl)furan] also known as furamidine. The biotransformation process of DB289 to DB75 in the human liver consists of three O-demet...

hylation reactions catalyzed by the Cyp4F enzyme subfamily and three N-dehydroxylation reactions catalyzed by cytrochrome b5 and NADH-cytochrome b5 reductase. DB289 was studied for therapeutic treatment against human African trypanosomiasis, Pneumocystis pneumonia and malaria. In November 2006, Immtech Pharmaceuticals, Inc. announced that the U.S. Food and Drug Administration (FDA) had granted orphan drug designation for pafuramidine (DB289) to treat Pneumocystis jiroveci pneumonia (PCP), a common life-threatening opportunistic infection in HIV/AIDS and other immunosuppressed patients. Despite the high efficacy of DB289 in patients, the mechanism of action of DB75 is unknown. The mechanism of antimicrobial activity of diamidine compounds is incompletely understood. They undergo active uptake by purine transporter systems in trypanosomes and their mechanism of action may involve interference with DNA-associated enzymes inhibition of heme crystallization11 or/and collapse of the transmitochondrial membrane potential.

PAFURAMIDINE MALEATE

K27F04K3A9

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

NADH-cytochrome b5 reductase

Cytochrome P450 4F2

Docosahexaenoic acid omega-hydroxylase CYP4F3

Protein-arginine N-methyltransferase 1

Quinone reductase 2

Conditions:

Pneumocystis pneumonia

African trypanosomiasis

Pafuramidine or DB289, [2,5-bis-(4-amidinophenyl)furan bis-O-methylamidoxime] is a pro-drug of DB75, [2,5-bis(4-amidinophenyl)furan] also known as furamidine. The biotransformation process of DB289 to DB75 in the human liver consists of three O-demet...

hylation reactions catalyzed by the Cyp4F enzyme subfamily and three N-dehydroxylation reactions catalyzed by cytrochrome b5 and NADH-cytochrome b5 reductase. DB289 was studied for therapeutic treatment against human African trypanosomiasis, Pneumocystis pneumonia and malaria. In November 2006, Immtech Pharmaceuticals, Inc. announced that the U.S. Food and Drug Administration (FDA) had granted orphan drug designation for pafuramidine (DB289) to treat Pneumocystis jiroveci pneumonia (PCP), a common life-threatening opportunistic infection in HIV/AIDS and other immunosuppressed patients. Despite the high efficacy of DB289 in patients, the mechanism of action of DB75 is unknown. The mechanism of antimicrobial activity of diamidine compounds is incompletely understood. They undergo active uptake by purine transporter systems in trypanosomes and their mechanism of action may involve interference with DNA-associated enzymes inhibition of heme crystallization11 or/and collapse of the transmitochondrial membrane potential.

PUTRESCINE DIHYDROCHLORIDE

X45SUR7RHY

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Protein-arginine N-methyltransferase 1

Ornithine decarboxylase

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