4-amino-PGA
4-amino-PGA Uses, Dosage, Side Effects, Food Interaction and all others data.
4-amino-PGA is an amino derivative of folic acid, which was once used as an antineoplastic agent in the treatment of pediatric leukemia. In the 1950's its production was discontinued in favor of methotrexate, which is less potent but less toxic. Off label, aminopterin has also been used in the treatment of psoriasis. Clinicians need to be aware of the characteristic teratologic effects of aminopterin and methotrexate.
| Trade Name | 4-amino-PGA |
| Generic | Aminopterin |
| Aminopterin Other Names | 4-amino-PGA, 4-aminofolic acid, Aminopteridine, Aminopterine, APGA, Minopterin, Pteramina |
| Type | |
| Formula | C19H20N8O5 |
| Weight | Average: 440.4127 Monoisotopic: 440.15566579 |
| Groups | Investigational, Withdrawn |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Prior to its withdrawal, aminopterin was initially used in the treatment of childhood leukemia; specifically to induce remissions. Later, aminopterin was used off-label in the United States to treat psoriasis, yielding dramatic lesion clearing. 4-amino-PGA was later supplanted by methotrexate for treating cancer because of its better therapeutic index. 4-amino-PGA (as well as methotrexate) has also been explored for use as an abortifacient. However, their association with severe congenital malformations and teratogenic effects have become known as fetal aminopterin syndrome.
How 4-amino-PGA works
4-amino-PGA is an amino derivative of folic acid which binds competitively to the dihydrofolate reductase enzyme to block tetrahydrofolate synthesis. Tetrahydrofolate is essential in the production of purines and pyrimadines, thus it's deficiency results in a reduction of DNA, RNA and protein synthesis.
Innovators Monograph
You find simplified version here 4-amino-PGA
