Rislenemdaz

Rislenemdaz
IUPAC ime
	4-Metilbenzil (3S,4R)-3-fluoro-4-[(2-pirimidinilamino)metil]-1-piperidinkarboksilat
Klinički podaci
Način primene	oralno
Identifikatori
CAS broj	808732-98-1
PubChem	CID 11394238
ChemSpider	9569140
UNII	5HAM167S5T
KEGG	D11340
ChEMBL	CHEMBL2068839
Sinonimi	CERC-301; MK-0657
Hemijski podaci
Formula	C19H23FN4O2
Molarna masa	358,42 g·mol−1
	SMILES CC1=CC=C(C=C1)COC(=O)N2CC[C@@H]([C@@H](C2)F)CNC3=NC=CC=N3; ;
	InChI InChI=1S/C19H23FN4O2/c1-14-3-5-15(6-4-14)13-26-19(25)24-10-7-16(17(20)12-24)11-23-18-21-8-2-9-22-18/h2-6,8-9,16-17H,7,10-13H2,1H3,(H,21,22,23)/t16-,17-/m1/s1; Key:RECBFDWSXWAXHY-IAGOWNOFSA-N;

Rislenemdaz (razvojni kodni naziv CERC-301, MK-0657) je oralno aktivni, selektivni antagonist podjedinice 2B NMDA receptora (NR2B) koji je u razvoju od strane Cerekora u Sjedinjenim Državama kao pomoćna terapija za depresiju otpornu na lečenje (TRD).^[1] U novembru 2013. su započeta klinička ispitivanja faze II,^[2] i istog meseca, rislenemdaz je dobio oznaku brze staze od Uprave za hranu i lekove za TRD.^[3]

Pilot studija je objavljena 2012. godine,^[1] i ispitivanje faze II je završeno 2014. godine, ali se smatralo nedovoljnim.^[4] Drugi pokušaj ispitivanja faze II 2016. takođe je otkrio da lek nije pokazao efikasnost protiv depresije.^[5]

Reference

^ ^а ^б Ibrahim L, Diaz Granados N, Jolkovsky L, Brutsche N, Luckenbaugh DA, Herring WJ, et al. (август 2012). „A Randomized, placebo-controlled, crossover pilot trial of the oral selective NR2B antagonist MK-0657 in patients with treatment-resistant major depressive disorder”. Journal of Clinical Psychopharmacology. 32 (4): 551—557. PMC 3438886  . PMID 22722512. doi:10.1097/JCP.0b013e31825d70d6.
^ „Cerecor Announces Initiation of Phase 2 Study for CERC-301, an Oral Rapid-acting Antidepressant Candidate”. Yahoo! Finance. 2013. Архивирано из оригинала 14. 7. 2014. г.
^ „Cerecor Receives Fast Track Designation for CERC-301 for the Treatment of Major Depressive Disorder”. Yahoo! Finance. 2013. Архивирано из оригинала 14. 7. 2014. г.
^ Clinical Trials NCT01941043 A Randomized, Double-Blind, Placebo-Controlled, Sequential Parallel Study of CERC-301 in the Adjunctive Treatment of Subjects With Severe Depression and Recent Active Suicidal Ideation Despite Antidepressant Treatment
^ „Cerecor (CERC) Announces CERC-301 Phase 2 Missed Primary Endpoint in MDD”. streetinsider.com.

Spoljašnje veze

CERC-301 - Cerecor, Inc. Архивирано на сајту Wayback Machine (20. октобар 2016)
CERC-301 - AdisInsight

[pmid22722512-1] а ^б Ibrahim L, Diaz Granados N, Jolkovsky L, Brutsche N, Luckenbaugh DA, Herring WJ, et al. (август 2012). „A Randomized, placebo-controlled, crossover pilot trial of the oral selective NR2B antagonist MK-0657 in patients with treatment-resistant major depressive disorder”. Journal of Clinical Psychopharmacology. 32 (4): 551—557. PMC 3438886  . PMID 22722512. doi:10.1097/JCP.0b013e31825d70d6.

[YahooFinance2013a-2] „Cerecor Announces Initiation of Phase 2 Study for CERC-301, an Oral Rapid-acting Antidepressant Candidate”. Yahoo! Finance. 2013. Архивирано из оригинала 14. 7. 2014. г.

[YahooFinance2013b-3] „Cerecor Receives Fast Track Designation for CERC-301 for the Treatment of Major Depressive Disorder”. Yahoo! Finance. 2013. Архивирано из оригинала 14. 7. 2014. г.

[4] Clinical Trials NCT01941043 A Randomized, Double-Blind, Placebo-Controlled, Sequential Parallel Study of CERC-301 in the Adjunctive Treatment of Subjects With Severe Depression and Recent Active Suicidal Ideation Despite Antidepressant Treatment

[streetinsider-5] „Cerecor (CERC) Announces CERC-301 Phase 2 Missed Primary Endpoint in MDD”. streetinsider.com.

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