Tabimorelin

Tabimorelin
IUPAC ime
	N-[(2E)-5-amino-5-metilheks-enoil]-N-metil-3-(2-naftil)alanil-N,Nα-dimetil-D-fenilalaninamid
Identifikatori
ATC kod	none
PubChem	CID 9810101
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)
Hemijski podaci
Formula	C32H40N4O3
Molarna masa	528,683 g/mol
	SMILES c3c1ccccc1ccc3CC(N(C)C(=O)C=CCC(N)(C)C)C(=O)N(C)C(C(=O)NC)Cc2ccccc2; ;

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.^[1] 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.^[2]^[3] Međutim, kliničko dejstvo na deficit hormona rasta odraslih osoba je ograničen. Samo pacijenti sa najtežim GH-deficitom su pokazali poboljšanje,^[4] i utvrđeno je da tabimorelin deluje kao CYP3A4 inhibitor te da stoga može da izazove nepoželjne interakcije sa drugim lekovima.^[5]

Vidi još

Reference

^ Hansen, B. S.; Raun, K.; Nielsen, K. K.; Johansen, P. B.; Hansen, T. K.; Peschke, B.; Lau, J.; Andersen, P. H.; Ankersen, M. (1999). „Pharmacological characterisation of a new oral GH secretagogue, NN703”. European Journal of Endocrinology. 10427162 (2): 180—189. PMID 10427162. doi:10.1530/eje.0.1410180.
^ Zdravkovic, M.; Søgaard, B.; Ynddal, L.; Christiansen, T.; Agersø, H.; Thomsen, M. S.; Falch, J. E.; Ilondo, M. M. (2000). „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 & Igf Research : Official Journal of the Growth Hormone Research Society and the International Igf Research Society. 11032702 (4): 193—198. PMID 11032702. doi:10.1054/ghir.2000.0152.
^ Zdravkovic, M.; Christiansen, T.; Eliot, L.; Agersoe, H.; Thomsen, M. S.; Falch, J. F.; Søgaard, B.; Ynddal, L.; Ilondo, M. M. (2001). „The pharmacokinetics, pharmacodynamics, safety and tolerability following 7 days daily oral treatment with NN703 in healthy male subjects”. Growth Hormone & Igf Research : Official Journal of the Growth Hormone Research Society and the International Igf Research Society. 11437473 (1): 41—48. PMID 11437473. doi:10.1054/ghir.2000.0188.
^ Svensson, J.; Monson, J. P.; Vetter, T.; Hansen, T. K.; Savine, R.; Kann, P.; Bex, M.; Reincke, M.; Hagen, C.; Beckers, A.; Ilondo, M. M.; Zdravkovic, M.; Bengtsson, B. A.; Korbonits, M.; NN703 Clinical Research Group (2003). „Oral administration of the growth hormone secretagogue NN703 in adult patients with growth hormone deficiency”. Clinical Endocrinology. 12699438 (5): 572—580. PMID 12699438. S2CID 33510538. doi:10.1046/j.1365-2265.2003.01754.x.
^ Zdravkovic, M.; Olsen, A. K.; Christiansen, T.; Schulz, R.; Taub, M. E.; Thomsen, M. S.; Rasmussen, M. H.; Ilondo, M. M. (2003). „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. 12610745 (10): 683—688. PMID 12610745. S2CID 22546247. doi:10.1007/s00228-002-0539-1.

Spoljašnje veze

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[1] Hansen, B. S.; Raun, K.; Nielsen, K. K.; Johansen, P. B.; Hansen, T. K.; Peschke, B.; Lau, J.; Andersen, P. H.; Ankersen, M. (1999). „Pharmacological characterisation of a new oral GH secretagogue, NN703”. European Journal of Endocrinology. 10427162 (2): 180—189. PMID 10427162. doi:10.1530/eje.0.1410180.

[2] Zdravkovic, M.; Søgaard, B.; Ynddal, L.; Christiansen, T.; Agersø, H.; Thomsen, M. S.; Falch, J. E.; Ilondo, M. M. (2000). „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 & Igf Research : Official Journal of the Growth Hormone Research Society and the International Igf Research Society. 11032702 (4): 193—198. PMID 11032702. doi:10.1054/ghir.2000.0152.

[3] Zdravkovic, M.; Christiansen, T.; Eliot, L.; Agersoe, H.; Thomsen, M. S.; Falch, J. F.; Søgaard, B.; Ynddal, L.; Ilondo, M. M. (2001). „The pharmacokinetics, pharmacodynamics, safety and tolerability following 7 days daily oral treatment with NN703 in healthy male subjects”. Growth Hormone & Igf Research : Official Journal of the Growth Hormone Research Society and the International Igf Research Society. 11437473 (1): 41—48. PMID 11437473. doi:10.1054/ghir.2000.0188.

[4] Svensson, J.; Monson, J. P.; Vetter, T.; Hansen, T. K.; Savine, R.; Kann, P.; Bex, M.; Reincke, M.; Hagen, C.; Beckers, A.; Ilondo, M. M.; Zdravkovic, M.; Bengtsson, B. A.; Korbonits, M.; NN703 Clinical Research Group (2003). „Oral administration of the growth hormone secretagogue NN703 in adult patients with growth hormone deficiency”. Clinical Endocrinology. 12699438 (5): 572—580. PMID 12699438. S2CID 33510538. doi:10.1046/j.1365-2265.2003.01754.x.

[5] Zdravkovic, M.; Olsen, A. K.; Christiansen, T.; Schulz, R.; Taub, M. E.; Thomsen, M. S.; Rasmussen, M. H.; Ilondo, M. M. (2003). „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. 12610745 (10): 683—688. PMID 12610745. S2CID 22546247. doi:10.1007/s00228-002-0539-1.

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