Tabimorelin

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Tabimorelin
(IUPAC) ime
N-[(2E)-5-amino-5-metilheks-enoil]-N-metil-3-(2-naftil)alanil-N,Nα-dimetil-D-fenilalaninamid
Klinički podaci
Identifikatori
ATC kod nije dodeljen
PubChem[1][2] 9810101
Hemijski podaci
Formula C32H40N4O3 
Mol. masa 528,683 g/mol
SMILES eMolekuli & PubHem
Sinonimi ((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)
Farmakoinformacioni podaci
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Pravni status

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]

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Reference[uredi - уреди]

  1. 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
  2. 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. 
  3. 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
  4. 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
  5. 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
  6. 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
  7. 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

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