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. 2021 Mar 18;24(6):450–463. doi: 10.1093/ijnp/pyab013

Table 3.

Effect of V1B receptor antagonists in clinical trials (depression)

Compound Trial Dose regimen Patients Primary endpoint Results ClinicalTrial.gov identifier Reference
SSR149415 Randomized, double-blinded, placebo-controlled study (DFI5878) SSR149415 (100 mg, 250 mg) or placebo, BID for 8 wk (active control: escitalopram, 10 mg QD) MDD patients SSR149415 100 mg (n = 80) SSR149415 250 mg (n = 79) placebo n = 75 escitalopram n = 84 Changes from baseline HDRS total score at wk 8 • SSR149415 (250 but not 100 mg) had significantly greater reductions in HDRS changes from baseline compared with placebo, while escitalopram had nonsignificant reduction in HDRS
• Similar trends of greater improvements in SSR149415 observed in secondary endpoints (CGI-S, MADRS), while these effects did not reach statistical significance
NCT00358631 Griebel et al., 2012
Randomized, double-blinded, placebo-controlled study (DFI5879) SSR149415 (100 mg, 250 mg) or placebo, BID for 8 wk (active control: paroxetine, 20 mg QD) MDD patients SSR149415 100 mg (n = 82) SSR149415
250 mg (n = 81)
placebo n = 77
escitalopram n = 80
Changes from baseline HDRS total score at wk 8 • Differences between placebo and each SSR149415 dose on HDRS score not statistically significant, while paroxetine significantly reduced HDRS score
• No statistical difference between placebo and each SSR149414 dose on secondary endpoints (CGI-S, MADRS).
NCT00361491
Randomized, double-blinded, placebo-controlled study (PDY5467) SSR149415 (100 mg, 250 mg) or placebo, BID for 4 wk MDD patients SSR149415 100 mg (n = 25) SSR149415 250 mg (n = 24) placebo n = 24 Plasma cortisol concentration response to CRF administration before and after 27 d dosing • Differences between placebo and each SSR149415 dose on primary endpoint not statistically significant
• SSR149415 group showed greater mean improvements from baseline HDRS score and CGI-S than placebo group, although differences not statistically significant
NCT01606384
ABT-436 Randomized, double-blinded, placebo-controlled study ABT-436 (800 mg) or placebo, QD for 7 d MDD patients ABT-436 800 mg (n = 31) placebo n = 20 Basal HPA parameters at d 7 • Basal HPA parameters (urine total glucocorticoids, plasma ACTH, urine/serum/ saliva cortisol, etc.) lower in ABT-436 group than in placebo group
• Dynamic HPA parameters (plasma ACTH and serum cortisol response to CRF) lower in ABT- 436 group than in placebo group
• ABT-436 had favorable symptom responses on 2 of 5 MASQ subscale compared with placebo but no differences on HDRS score
NCT01380704 Katz et al., 2017
TS-121 Randomized, double-blinded, placebo-controlled study TS-121 (10 mg, 50 mg) or placebo, QD for 6 wk (adjunctive treatment) MDD patients with inadequate response to current antidepressant treatment TS-121 10 mg (n = 16) TS-121 50 mg (n = 17) placebo n = 18 Changes from baseline MADRS score at wk 6 • TS-121 had greater reductions in MADRS change from baseline compared with placebo but changes not statistically significant
• Similar trends of non-significantly greater improvements in TS-121 observed in secondary endpoints (CGI-S, HAM-A, SDQ, etc.), but effects not statistically significant
• Higher baseline urinary and hair cortisol associated with greater separation between TS-121 and placebo in MADRS score
NCT03093025 Kamiya et al., 2020

Abbreviations: ACTH, adrenocorticotropic hormone; CGI-S, Clinical Global Impressions-Severity of Illness Score; CRF, corticotropin-releasing factor; HAM-A, Hamilton Anxiety Rating Scale; HDRS, Hamilton Depression Rating Scale; HPA, hypothalamus-pituitary-adrenal; MADRS, Montgomery-Åsberg Depression Rating Scale; MASQ, Mood and Anxiety Symptom Questionnaire; MDD, major depressive disorder; SDQ, Symptoms of Depression Questionnaire.