| Systematic (IUPAC) name | |
|---|---|
| (4R)-4-hydroxy-L-prolyl-N5-(diaminomethylidene)-L-ornithylglycyl-N-[(2S)-2-amino-3-(4-fluorophenyl)propanoyl]-L-tryptophanamide | |
| Clinical data | |
| Pregnancy cat. | ? |
| Legal status | Non-regulated |
| Routes | Subcutaneous injection |
| Pharmacokinetic data | |
| Half-life | 15-30 minutes[1] |
| Identifiers | |
| CAS number | 173240-15-8 |
| ATC code | None |
| PubChem | CID 177265 |
| ChemSpider | 154356 |
| UNII | RO19OXA9NG |
| Chemical data | |
| Formula | C33H43FN10O6 |
| Mol. mass | 694.756 g/mol |
| SMILES | eMolecules & PubChem |
Nemifitide (INN-00835), also known as 4-F-Phe-4-OH-Pro-Arg-Gly-Trp-NH2, is a novel antidepressant drug with a pentapeptide structure similar to that of melanocyte-inhibiting factor (MIF-1).[1][2] It is under development by Tetragenex (previously Innapharma, Inc.) for the treatment of major depressive disorder.[3] It has been given to over 430 humans over the course of 12 clinical trials throughout a little over the past decade, and has reached Phase III studies, but has not yet been approved for marketing in any country.[3]
Nemifitide has shown mixed efficacy in alleviating depressive symptoms,[4][5] but in the cases in which it has worked, it has proven to have a rapid onset of action (~5-7 days), few to no side effects, and an excellent safety profile.[5] However, it is inactive orally, and must be administered via subcutaneous injection (SC). Remarkably, despite having a very short half-life of only 15-30 minutes,[1] in most or all studies assessing its efficacy, it has been administered merely once daily via the SC route, and yet is as effective as it is against depression.
Its mechanism of action is unclear, but since MIF-1 has been demonstrated to have similar antidepressant effects,[6] it may act in an analogous manner.[1][2] Of interest, however, is that nemifitide binds to several receptors at micromolar concentrations, including 5-HT2A, NPY1, bombesin, and melanocortin MC4 and MC5.[5] In addition, it has been determined to act in an antagonistic manner at the 5-HT2A receptor.[5] However, it is unclear whether any of these relatively weak actions are of significance.