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Tabimorelin
Tabimorelin
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| (IUPAC) ime
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| N-[(2E)-5-amino-5-metilheks-enoil]-N-metil-3-(2-naftil)alanil-N,Nα-dimetil-D-fenilalaninamid
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| Klinički podaci
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| Identifikatori
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| ATC kod
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nije dodeljen
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| PubChem[1][2]
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9810101
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| Hemijski podaci
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| Formula
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C32H40N4O3
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| Mol. masa
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528,683 g/mol
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| SMILES
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eMolekuli & PubHem
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| InChI |
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InChI=1S/C32H40N4O3/c1-32(2,33)19-11-16-29(37)35(4)28(22-24-17-18-25-14-9-10-15-26(25)20-24)31(39)36(5)27(30(38)34-3)21-23-12-7-6-8-13-23/h6-18,20,27-28H,19,21-22,33H2,1-5H3,(H,34,38)/b16-11+/t27-,28-/m1/s1  Y
Key: WURGZWOTGMLDJP-ZCYANPAGSA-N Y |
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| Sinonimi
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((2E)-5-amino-5-metilheks-2-enoinska kiselina N-metil-N-((1R)-1-(N-metil-N-((1R)-1-(metilkarbamoil)-2-feniletil)karbamoil)-2-(2-naftil)etil)amid)
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| Farmakoinformacioni podaci
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| Trudnoća
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?
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| Pravni status
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Tabimorelin (NN-703) je lek koji deluje kao potentan, oralno aktivan stimulator izlučivanja hormona rasta koji oponaša dejstvo endogenog peptidnog agonista grelina. On je bio jedan od prvih GH izlučivača. U velikoj meri je sličan polipeptidu, mada je oralno aktivan.[3] Tabimorelin proizvodi znatna povećanja nivoa faktora rasta i IGF-1, zajedno sa manjim prolaznim povećanjem nivoa drugih hormona kao što su ACTH, kortizol i prolaktin.[4][5] Međutim, kliničko dejstvo na deficit hormona rasta odraslih osoba je ograničen. Samo pacijenti sa najtežim GH-deficitom su pokazali poboljšanje,[6] i utvrđeno je da tabimorelin deluje kao CYP3A4 inhibitor te da stoga može da izazove nepoželjne interakcije sa drugim lekovima.[7]
Povezano
Reference
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Hansen BS, Raun K, Nielsen KK, Johansen PB, Hansen TK, Peschke B, Lau J, Andersen PH, Ankersen M. Pharmacological characterisation of a new oral GH secretagogue, NN703. European Journal of Endocrinology. 1999 Aug;141(2):180-9. PMID 10427162
- ↑ Zdravkovic M, Søgaard B, Ynddal L, Christiansen T, Agersø H, Thomsen MS, Falch JE, Ilondo MM. The pharmacokinetics, pharmacodynamics, safety and tolerability of a single dose of NN703, a novel orally active growth hormone secretagogue in healthy male volunteers. Growth Hormone and IGF Research. 2000 Aug;10(4):193-8. PMID 11032702
- ↑ Zdravkovic M, Christiansen T, Eliot L, Agersoe H, Thomsen MS, Falch JF, Søgaard B, Ynddal L, Ilondo MM. The pharmacokinetics, pharmacodynamics, safety and tolerability following 7 days daily oral treatment with NN703 in healthy male subjects. Growth Hormone and IGF Research. 2001 Feb;11(1):41-8. PMID 11437473
- ↑ Svensson J, Monson JP, Vetter T, Hansen TK, Savine R, Kann P, Bex M, Reincke M, Hagen C, Beckers A, Ilondo MM, Zdravkovic M, Bengtsson BA, Korbonits M; NN703 Clinical Research Group. Oral administration of the growth hormone secretagogue NN703 in adult patients with growth hormone deficiency. Clinical Endocrinology. 2003 May;58(5):572-80. PMID 12699438
- ↑ Zdravkovic M, Olsen AK, Christiansen T, Schulz R, Taub ME, Thomsen MS, Rasmussen MH, Ilondo MM. A clinical study investigating the pharmacokinetic interaction between NN703 (tabimorelin), a potential inhibitor of CYP3A4 activity, and midazolam, a CYP3A4 substrate. European Journal of Clinical Pharmacology. 2003 Feb;58(10):683-8. PMID 12610745
Vanjske veze
Šablon:Neuropeptidni ligandi
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