Inxight Drugs

U.S. Department of Health & Human Services Divider Arrow

National Institutes of Health Divider Arrow

NCATS

Return Home Inxight Drugs

Home
Browse Drugs
Search
- Structure Search
- Sequence Search
Downloads
About

Show Filters

Hide Filters

Condition

Pediatric leukemia

2

Unknown

2,578

Pain

614

Cancer

592

Hypertension

567

All Match

Any Match

Exclude Selected

Exclude Selected

Development Status

US Previously Marketed

2

All Match

Any Match

Exclude Selected

Exclude Selected

Primary Target

Dihydrofolate reductase

2

Folylpoly-gamma-glutamate synthetase

2

All Match

Any Match

Exclude Selected

Exclude Selected

Highest Phase

Approved

2

All Match

Any Match

Exclude Selected

Exclude Selected

Approval Year

1952

2

All Match

Any Match

Exclude Selected

Exclude Selected

Treatment Modality

Primary

2

All Match

Any Match

Exclude Selected

Exclude Selected

Originator

Lederle

2

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Class

Chemical

2

All Match

Any Match

Exclude Selected

Exclude Selected

Code System

CAS

2

EVMPD

2

FDA UNII

2

NCI_THESAURUS

2

NSC

2

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Form

Principal Form

1

Salts, Hydrates, Esters, etc.

1

All Match

Any Match

Exclude Selected

Exclude Selected

Showing 1 - 2 of 2 results

First page disabled
Previous page disabled
1
Next page disabled
Next page disabled

AMINOPTERIN

JYB41CTM2Q

Export Data
Search for Structure

Status:

US Previously Marketed

First approved in 1952

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Dihydrofolate reductase

Folylpoly-gamma-glutamate synthetase

Conditions:

Acute lymphocytic leukemia

Endometrial cancer

Rheumatoid arthritis

Pediatric leukemia

Aminopterin is a synthetic derivative of pterins with antineoplastic and immunosuppressive properties. As a folate analog, aminopterin competes for the folate binding site of the enzyme dihydrofolate reductase, thereby blocking tetrahydrofolate synth...

esis, and resulting in depletion of nucleotide precursors and inhibition of DNA, RNA and protein synthesis. Aminopterin was marketed by Lederle Laboratories (Pearl River, New York) in the United States from 1953 to 1964 for the indication of pediatric leukemia. The closely related antifolate methotrexate was simultaneously marketed by the company during the same period. Aminopterin was discontinued by Lederle Laboratories in favor of methotrexate due to manufacturing difficulties of the former. During the period Aminopterin was marketed, the agent was used off-label to safely treat over 4,000 patients with psoriasis in the United States, producing dramatic clearing of lesions. The use of aminopterin in cancer treatment was supplanted in the 1950s by methotrexate due to the latter's better therapeutic index in a rodent tumor model. Now in a more pure preparation and supported by laboratory evidence of superior tumor cell uptake in vitro, aminopterin is being investigated in clinical trials in leukemia as a potentially superior antifolate to methotrexate.

AMINOPTERIN SODIUM

FZU1QI13O9

Export Data
Search for Structure

Status:

US Previously Marketed

First approved in 1952

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

Dihydrofolate reductase

Folylpoly-gamma-glutamate synthetase

Conditions:

Acute lymphocytic leukemia

Endometrial cancer

Rheumatoid arthritis

Pediatric leukemia

Aminopterin is a synthetic derivative of pterins with antineoplastic and immunosuppressive properties. As a folate analog, aminopterin competes for the folate binding site of the enzyme dihydrofolate reductase, thereby blocking tetrahydrofolate synth...

esis, and resulting in depletion of nucleotide precursors and inhibition of DNA, RNA and protein synthesis. Aminopterin was marketed by Lederle Laboratories (Pearl River, New York) in the United States from 1953 to 1964 for the indication of pediatric leukemia. The closely related antifolate methotrexate was simultaneously marketed by the company during the same period. Aminopterin was discontinued by Lederle Laboratories in favor of methotrexate due to manufacturing difficulties of the former. During the period Aminopterin was marketed, the agent was used off-label to safely treat over 4,000 patients with psoriasis in the United States, producing dramatic clearing of lesions. The use of aminopterin in cancer treatment was supplanted in the 1950s by methotrexate due to the latter's better therapeutic index in a rodent tumor model. Now in a more pure preparation and supported by laboratory evidence of superior tumor cell uptake in vitro, aminopterin is being investigated in clinical trials in leukemia as a potentially superior antifolate to methotrexate.

HHS VULNERABILITY DISCLOSURE

For language access assistance, contact the NCATS Public Information Officer

National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966


			version 1.1