The World Health Organization's ATC classification organizes medical drugs based on therapeutic properties, chemical composition, and anatomy. It helps make essential medicines readily available globally and is widely used in the pharmaceutical industry.
Level | Code | Title | |
---|---|---|---|
1 | L | Antineoplastic and immunomodulating agents | |
2 | L01 | Antineoplastic agents | |
3 | L01B | Antimetabolites | |
4 | L01BA | Folic acid analogues |
Code | Title | |
---|---|---|
L01BA01 | Methotrexate | |
L01BA03 | Raltitrexed | |
L01BA04 | Pemetrexed | |
L01BA05 |
Active Ingredient | Description | |
---|---|---|
Methotrexate |
Methotrexate (4-amino-10-methylfolic acid) is a folic acid antagonist which inhibits the reduction of folic acid and increase of tissue cells. Methotrexate enters the cell through an active transport mechanism of reduced folates. As a result of polyglutamation of methotrexate caused by the folylpolyglutamylate enzyme, the duration of the cytotoxic effect of the drug substance in the cell increases. |
|
Pemetrexed |
Pemetrexed is a folate analog metabolic inhibitor that exerts its action by disrupting folate-dependent metabolic processes essential for cell replication. In vitro studies have shown that pemetrexed inhibits thymidylate synthase (TS), dihydrofolate reductase (DHFR), glycinamide ribonucleotide formyltransferase (GARFT) and and to a lesser extent aminoimidazole carboxamide ribonucleotide formyltransferase (AICARFT), which are folate-dependent enzymes involved in the de novo biosynthesis of thymidine and purine nucleotides. Pemetrexed is taken into cells by membrane carriers such as the reduced folate carrier and membrane folate binding protein transport systems. Once in the cell, pemetrexed is converted to polyglutamate forms by the enzyme folylpolyglutamate synthetase. The polyglutamate forms are retained in cells and are inhibitors of TS and GARFT. Polyglutamation is a time- and concentration-dependent process that occurs in tumor cells and, is thought to occur to a lesser extent, in normal tissues. Polyglutamated metabolites are thought to have an increased intracellular half-life resulting in prolonged drug action in malignant cells. |
|
Pralatrexate |
Pralatrexate is a folate analog metabolic inhibitor that competitively inhibits dihydrofolate reductase. It is also a competitive inhibitor for polyglutamylation by the enzyme folylpolyglutamyl synthetase. This inhibition results in the depletion of thymidine and other biological molecules the synthesis of which depends on single carbon transfer. Pralatrexate is used for the treatment of patients with relapsed or refractory peripheral T-cell lymphoma (PTCL). |
|
Raltitrexed |
Raltitrexed is a folate analogue belonging to the family of anti-metabolites and has potent inhibitory activity against the enzyme thymidylate synthase (TS). Compared to other antimetabolites such as 5-fluorouracil or methotrexate, raltitrexed acts as a direct and specific TS inhibitor. TS is a key enzyme in the de novo synthesis of thymidine triphosphate (TTP), a nucleotide required exclusively for deoxyribonucleic acid (DNA) synthesis. Inhibition of TS leads to DNA fragmentation and cell death. |
Title | Information Source | Document Type | |
---|---|---|---|
ARMISARTE Concentrate for solution for infusion | European Medicines Agency (EU) | MPI, EU: SmPC | |
CIAMBRA Powder for concentrate for solution for infusion | European Medicines Agency (EU) | MPI, EU: SmPC | |
FOLOTYN Solution for injection | FDA, National Drug Code (US) | MPI, US: SPL/PLR | |
JYLAMVO Oral solution | European Medicines Agency (EU) | MPI, EU: SmPC | |
METHOTREXATE Solution for Injection | Medicines & Healthcare Products Regulatory Agency (GB) | MPI, EU: SmPC | |
METHOTREXATE Tablets | Medicines & Healthcare Products Regulatory Agency (GB) | MPI, EU: SmPC | |
METOJECT PEN Solution for injection in pre-filled pen | Medicines & Healthcare Products Regulatory Agency (GB) | MPI, EU: SmPC | |
TOMUDEX Powder for solution for infusion | Medicines & Healthcare Products Regulatory Agency (GB) | MPI, EU: SmPC |