Tesofenzin
Tesofenzin (NS2330) je inhibitor ponovnog preuzimanja serotonin–noradrenalin–dopamina iz feniltropanske porodice lekova, koji se razvija za lečenje gojaznosti.[1] Tesofenzin je prvobitno razvila danska biotehnološka kompanija NeuroSearch, koja je prenela prava na Sanionu 2014. godine.[2]
 | |
| IUPAC ime | |
|---|---|
(1R,2R,3S)-3-(3,4-dihlorofenil)-2-(etoksimetil)-8-metil-8-azabiciklo[3.2.1]oktan | |
| Klinički podaci | |
| Kategorija trudnoće |
|
| Način primene | Oralno |
| Pravni status | |
| Pravni status |
|
| Farmakokinetički podaci | |
| Bioraspoloživost | 90% |
| Metabolizam | 15–20% renalno; hepatički: CYP3A4 |
| Poluvreme eliminacije | 220 sata |
| Izlučivanje | Nije aplikabilno |
| Identifikatori | |
| CAS broj | 195875-84-4  |
| ATC kod | None |
| PubChem | CID 11370864 |
| ChemSpider | 9545781 |
| UNII | BLH9UKX9V1 |
| Hemijski podaci | |
| Formula | C17H23Cl2NO |
| Molarna masa | 328,28 g·mol−1 |
| |
| |
Prema podacima iz 2019. godine, razvoj tezofenzin je prekinut za lečenje Alchajmerove i Parkinsonove bolesti, ali je u fazi III kliničkog ispitivanja za gojaznost.[3]
Osobine
уредиTesofenzin je organsko jedinjenje, koje sadrži 17 atoma ugljenika i ima molekulsku masu od 328,277 Da.
| Osobina | Vrednost |
|---|---|
| Broj akceptora vodonika | 2 |
| Broj donora vodonika | 0 |
| Broj rotacionih veza | 4 |
| Particioni koeficijent[4] (ALogP) | 4,2 |
| Rastvorljivost[5] (logS, log(mol/L)) | -5,0 |
| Polarna površina[6] (PSA, Å2) | 12,5 |
Reference
уреди- ^ Doggrell SA. "Tesofensine – a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2009 372; 1906–13" Doggrell SA (јул 2009). „Tesofensine--a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2008;372:1906-13” (PDF). Expert Opinion on Investigational Drugs. 18 (7): 1043—6. PMID 19548858. S2CID 207475155. doi:10.1517/13543780902967632.
- ^ „NeuroSearch A/S signs agreement to transfer Phase I-II projects NS2359 and NS2330 (Tesofensine)”. NeuroSearch company announcement. Приступљено 30. 10. 2014.
- ^ „Tesofensine - Saniona”. AdisInsight. Springer Publishing. 29. 1. 2019. Приступљено 31. 10. 2019.
- ^ Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A. 102: 3762—3772. doi:10.1021/jp980230o.
- ^ Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488—1493. PMID 11749573. doi:10.1021/ci000392t.
- ^ Ertl P.; Rohde B.; Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714—3717. PMID 11020286. doi:10.1021/jm000942e.
Literatura
уреди- Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
- Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.
