Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C16H15FN6OS |
| Molecular Weight | 358.393 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
C[C@H]1N(CCN2C1=NN=C2C3=NC(C)=NS3)C(=O)C4=CC=C(F)C=C4
InChI
InChIKey=PPSNFPASKFYPMN-SECBINFHSA-N
InChI=1S/C16H15FN6OS/c1-9-13-19-20-14(15-18-10(2)21-25-15)23(13)8-7-22(9)16(24)11-3-5-12(17)6-4-11/h3-6,9H,7-8H2,1-2H3/t9-/m1/s1
| Molecular Formula | C16H15FN6OS |
| Molecular Weight | 358.393 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
CNS Activity
Originator
Approval Year
Sample Use Guides
Phase 2 study for the treatment of hot flashes (vasomotor symptoms) in postmenopausal women. The dose of ESN364 varies across 7 treatment groups, with groups receiving once a day or twice a day blinded study drug. Doses range from 30 mg to 180 mg total daily dosing for 12 weeks.
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 02:53:17 UTC 2023
by
admin
on
Sat Dec 16 02:53:17 UTC 2023
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| Record UNII |
83VNE45KXX
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| Record Status |
Validated (UNII)
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| Record Version |
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HI-226
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C171845
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DB15669
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FEZOLINETANT
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117604931
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DTXSID601103615
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100000174631
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1629229-37-3
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83VNE45KXX
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10205
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| Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
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ACTIVE MOIETY |
INTERVENTION(S): In part 1 of the study, men received single oral doses of 3-180 mg or placebo. In part 2, men received placebo or 20, 60, or 180 mg each day for 10 days. In part 3, women received placebo or 20, 60, or 180 mg each day for 21 days, where dosing was initiated on day 3 +/- 2 after menses.
RESULTS: ESN364 was well-tolerated and rapidly bioavailable with linear pharmacokinetics and no drug accumulation with repeated, daily oral administration. Drug treatment dose-dependently decreased basal LH, but not FSH, and consequently decreased estradiol and progesterone (in women) as well as testosterone (in men). The hormonal changes in women corresponded to delayed ovulation, decreased endometrial thickening, impeded follicular maturation, and prolongation of the menstrual cycle. Drug effects were rapidly reversible.
CONCLUSIONS: Oral administration of the NK3R antagonist, ESN364, suppressed the hypothalamic-pituitary-gonadal axis in healthy volunteers by selective modulation of gonadotropin secretion, leading to a restrained decrease in ovarian hormone levels in women. These results suggest that ESN364 may offer therapeutic benefit in the treatment of women's health disorders with a mitigated risk of menopausal-like adverse events.
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