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Details

Stereochemistry ABSOLUTE
Molecular Formula C21H34O2
Molecular Weight 318.4942
Optical Activity UNSPECIFIED
Defined Stereocenters 8 / 8
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BREXANOLONE

SMILES

CC(=O)[C@@]1([H])CC[C@@]2([H])[C@]3([H])CC[C@@]4([H])C[C@@]([H])(CC[C@]4(C)[C@@]3([H])CC[C@]12C)O

InChI

InChIKey=AURFZBICLPNKBZ-SYBPFIFISA-N
InChI=1S/C21H34O2/c1-13(22)17-6-7-18-16-5-4-14-12-15(23)8-10-20(14,2)19(16)9-11-21(17,18)3/h14-19,23H,4-12H2,1-3H3/t14-,15+,16-,17+,18-,19-,20-,21+/m0/s1

HIDE SMILES / InChI

Molecular Formula C21H34O2
Molecular Weight 318.4942
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 8 / 8
E/Z Centers 0
Optical Activity UNSPECIFIED

Allopregnanolone is a neurosteroid metabolite of progesterone. It is an allosteric modulator of inhibitory γ-aminobutyric acid (GABA-A) receptors on neural stem cells and other cell types in the brain. Allopregnanolone has effects similar to those of other positive allosteric modulators of the GABA action at GABAA receptor such as the benzodiazepines, including anxiolytic, sedative, and anticonvulsant activity. A solution of allopregnanolone, SAGE-547 is an intravenous allosteric modulator of both synaptic and extrasynaptic γ-aminobutyric acid type A (GABAA)receptors. It's believed that allopregnanolone is effective as an anticonvulsant when prolonged seizure activity has become resistant to benzodiazepine treatment. Under the names brexanolone and SAGE-547, allopregnanolone is under development by SAGE Therapeutics as an intravenously administered drug for the treatment of super-refractory status epilepticus, postpartum depression, and essential tremor. Allopregnanolone is in phase III trials for the treatment of super-refractory status epilepticus (SRSE) and postpartum depression.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Primary
Unknown

Approved Use

Unknown
Doses

Doses

DosePopulationAdverse events​
60 ug/kg/day 3 times / 60 hours multiple, intravenous
Recommended
Dose: 60 ug/kg/day, 3 times / 60 hours
Route: intravenous
Route: multiple
Dose: 60 ug/kg/day, 3 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 38
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 38
Sources:
Other AEs: Dizziness, Somnolence...
60 ug/kg/day 3 times / 60 hours multiple, intravenous
Recommended
Dose: 60 ug/kg/day, 3 times / 60 hours
Route: intravenous
Route: multiple
Dose: 60 ug/kg/day, 3 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 38
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 38
Sources:
Other AEs: Diarrhea, Dry mouth...
Other AEs:
Diarrhea (3%)
Dry mouth (11%)
Oropharyngeal pain (3%)
Loss of consciousness (5%)
Flush hot (5%)
Sources:
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
DLT: Loss of consciousness, Syncope...
Disc. AE: Loss of consciousness, Vertigo...
Dose limiting toxicities:
Loss of consciousness
Syncope
Somnolence
Dizziness
Fatigue
Infusion related reaction
Change in blood pressure
AEs leading to
discontinuation/dose reduction:
Loss of consciousness
Vertigo
Syncope
Presyncope
Infusion site pain
Sources:
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Other AEs: Tachycardia, Diarrhea...
Other AEs:
Tachycardia (2%)
Diarrhea (2%)
Dry mouth (3%)
Dyspepsia (2%)
Oropharyngeal pain (2%)
Dizziness (12%)
Loss of consciousness (3%)
Somnolence (13%)
Flush hot (2%)
Sources:
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Other AEs: Dizziness, Nausea...
Other AEs:
Dizziness (grade 1, 20%)
Nausea (grade 1, 10%)
Rash (grade 1, 10%)
Somnolence (grade 1-2, 20%)
Dizziness postural (grade 1, 10%)
Dry mouth (grade 1, 10%)
Hot flush (grade 1, 10%)
Pyrexia (grade 1, 10%)
Sedation (grade 1, 10%)
Sinus tachycardia (grade 2, 10%)
Vertigo (grade 1, 10%)
Sources:
270 ug/kg/day 1 times / day single, intravenous
Highest studied dose
Dose: 270 ug/kg/day, 1 times / day
Route: intravenous
Route: single
Dose: 270 ug/kg/day, 1 times / day
Sources:
healthy, adult
n = 32
Health Status: healthy
Age Group: adult
Population Size: 32
Sources:
Other AEs: Somnolence, Feeling of relaxation...
Other AEs:
Somnolence (93.7%)
Feeling of relaxation (9.4%)
Feeling abnormal (6.3%)
Psychomotor retardation (3.1%)
Euphoric mood (12.5%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Dizziness grade 1, 13%
60 ug/kg/day 3 times / 60 hours multiple, intravenous
Recommended
Dose: 60 ug/kg/day, 3 times / 60 hours
Route: intravenous
Route: multiple
Dose: 60 ug/kg/day, 3 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 38
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 38
Sources:
Somnolence grade 1, 21%
60 ug/kg/day 3 times / 60 hours multiple, intravenous
Recommended
Dose: 60 ug/kg/day, 3 times / 60 hours
Route: intravenous
Route: multiple
Dose: 60 ug/kg/day, 3 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 38
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 38
Sources:
Dry mouth 11%
60 ug/kg/day 3 times / 60 hours multiple, intravenous
Recommended
Dose: 60 ug/kg/day, 3 times / 60 hours
Route: intravenous
Route: multiple
Dose: 60 ug/kg/day, 3 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 38
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 38
Sources:
Diarrhea 3%
60 ug/kg/day 3 times / 60 hours multiple, intravenous
Recommended
Dose: 60 ug/kg/day, 3 times / 60 hours
Route: intravenous
Route: multiple
Dose: 60 ug/kg/day, 3 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 38
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 38
Sources:
Oropharyngeal pain 3%
60 ug/kg/day 3 times / 60 hours multiple, intravenous
Recommended
Dose: 60 ug/kg/day, 3 times / 60 hours
Route: intravenous
Route: multiple
Dose: 60 ug/kg/day, 3 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 38
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 38
Sources:
Flush hot 5%
60 ug/kg/day 3 times / 60 hours multiple, intravenous
Recommended
Dose: 60 ug/kg/day, 3 times / 60 hours
Route: intravenous
Route: multiple
Dose: 60 ug/kg/day, 3 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 38
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 38
Sources:
Loss of consciousness 5%
60 ug/kg/day 3 times / 60 hours multiple, intravenous
Recommended
Dose: 60 ug/kg/day, 3 times / 60 hours
Route: intravenous
Route: multiple
Dose: 60 ug/kg/day, 3 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 38
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 38
Sources:
Change in blood pressure DLT
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Dizziness DLT
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Fatigue DLT
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Infusion related reaction DLT
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Loss of consciousness DLT
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Somnolence DLT
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Syncope DLT
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Infusion site pain Disc. AE
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Loss of consciousness Disc. AE
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Presyncope Disc. AE
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Syncope Disc. AE
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Vertigo Disc. AE
75 ug/kg/day multiple, intravenous (mean)
Recommended
Dose: 75 ug/kg/day
Route: intravenous
Route: multiple
Dose: 75 ug/kg/day
Sources:
unhealthy, 18 to 45 years
n = 140
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 140
Sources:
Dizziness 12%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Somnolence 13%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Diarrhea 2%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Dyspepsia 2%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Flush hot 2%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Oropharyngeal pain 2%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Tachycardia 2%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Dry mouth 3%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Loss of consciousness 3%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 18 to 45 years
n = 102
Health Status: unhealthy
Condition: postpartum depression
Age Group: 18 to 45 years
Sex: F
Population Size: 102
Sources:
Dizziness postural grade 1, 10%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Dry mouth grade 1, 10%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Hot flush grade 1, 10%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Nausea grade 1, 10%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Pyrexia grade 1, 10%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Rash grade 1, 10%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Sedation grade 1, 10%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Vertigo grade 1, 10%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Dizziness grade 1, 20%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Somnolence grade 1-2, 20%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Sinus tachycardia grade 2, 10%
90 ug/kg/day 5 times / 60 hours multiple, intravenous
Recommended
Dose: 90 ug/kg/day, 5 times / 60 hours
Route: intravenous
Route: multiple
Dose: 90 ug/kg/day, 5 times / 60 hours
Sources:
unhealthy, 20 to 40 years
n = 10
Health Status: unhealthy
Condition: postpartum depression
Age Group: 20 to 40 years
Sex: F
Population Size: 10
Sources:
Euphoric mood 12.5%
270 ug/kg/day 1 times / day single, intravenous
Highest studied dose
Dose: 270 ug/kg/day, 1 times / day
Route: intravenous
Route: single
Dose: 270 ug/kg/day, 1 times / day
Sources:
healthy, adult
n = 32
Health Status: healthy
Age Group: adult
Population Size: 32
Sources:
Psychomotor retardation 3.1%
270 ug/kg/day 1 times / day single, intravenous
Highest studied dose
Dose: 270 ug/kg/day, 1 times / day
Route: intravenous
Route: single
Dose: 270 ug/kg/day, 1 times / day
Sources:
healthy, adult
n = 32
Health Status: healthy
Age Group: adult
Population Size: 32
Sources:
Feeling abnormal 6.3%
270 ug/kg/day 1 times / day single, intravenous
Highest studied dose
Dose: 270 ug/kg/day, 1 times / day
Route: intravenous
Route: single
Dose: 270 ug/kg/day, 1 times / day
Sources:
healthy, adult
n = 32
Health Status: healthy
Age Group: adult
Population Size: 32
Sources:
Feeling of relaxation 9.4%
270 ug/kg/day 1 times / day single, intravenous
Highest studied dose
Dose: 270 ug/kg/day, 1 times / day
Route: intravenous
Route: single
Dose: 270 ug/kg/day, 1 times / day
Sources:
healthy, adult
n = 32
Health Status: healthy
Age Group: adult
Population Size: 32
Sources:
Somnolence 93.7%
270 ug/kg/day 1 times / day single, intravenous
Highest studied dose
Dose: 270 ug/kg/day, 1 times / day
Route: intravenous
Route: single
Dose: 270 ug/kg/day, 1 times / day
Sources:
healthy, adult
n = 32
Health Status: healthy
Age Group: adult
Population Size: 32
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 17 uM]
no [IC50 49 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no [IC50 >100 uM]
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
no
yes [IC50 0.41 uM]
yes [IC50 0.41 uM]
yes [Inhibition 2 uM]
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
yes
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
unlikely
unlikely
unlikely
unlikely
unlikely
unlikely
yes
yes
yes
yes
yes
yes
Tox targets
PubMed

PubMed

TitleDatePubMed
Increase in the cerebrospinal fluid content of neurosteroids in patients with unipolar major depression who are receiving fluoxetine or fluvoxamine.
1998 Mar 17
Social isolation-induced changes in the hypothalamic-pituitary-adrenal axis in the rat.
2005 Dec
Gonadotropin stimulation of steroid synthesis and metabolism in the Rana pipiens ovarian follicle: sequential changes in endogenous steroids during ovulation, fertilization and cleavage stages.
2006 May
In silico prediction of pregnane X receptor activators by machine learning approaches.
2007 Jan
Fecal steroid metabolites and reproductive monitoring in a female Tsushima leopard cat (Prionailurus bengalensis euptilurus).
2010 Nov
The bile acid receptor TGR5 (Gpbar-1) acts as a neurosteroid receptor in brain.
2010 Nov 15
Chronic ethanol exposure produces tolerance to elevations in neuroactive steroids: mechanisms and reversal by exogenous ACTH.
2010 Oct
Patents

Sample Use Guides

Subjects will receive and intravenous infusion of Allopregnanolone at escalating doses of 2mg, 4mg, and 6mg once weekly over a three week period. The highest dose tolerated without sedation will be held stable for the remaining weekly infusions, for a total of 12 infusions.
Route of Administration: Intravenous
GABA-induced current was enhanced by allopregnanolone at concentrations of 0.01 uM and more in guinea-pig adrenal medullary cells.
Substance Class Chemical
Created
by admin
on Sat Jun 26 16:06:16 UTC 2021
Edited
by admin
on Sat Jun 26 16:06:16 UTC 2021
Record UNII
S39XZ5QV8Y
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BREXANOLONE
INN   USAN  
Official Name English
ALLOPREGNAN-3.ALPHA.-OL-20-ONE [MI]
Common Name English
BREXANOLONE [INN]
Common Name English
ALLOTETRAHYDROPROGESTERONE
Common Name English
BREXANOLONE [WHO-DD]
Common Name English
3.ALPHA.-HYDROXY-5.ALPHA.-PREGNAN-20-ONE
Systematic Name English
BREXANOLONE [ORANGE BOOK]
Common Name English
PREGNAN-20-ONE, 3-HYDROXY-, (3.ALPHA.,5.ALPHA.)-
Systematic Name English
SGE-102
Code English
(+)-3.ALPHA.-HYDROXY-5.ALPHA.-PREGNAN-20-ONE
Systematic Name English
ALLOPREGNAN-3.ALPHA.-OL-20-ONE
MI  
Common Name English
BREXANOLONE [USAN]
Common Name English
ALLOPREGNANOLONE
Common Name English
SAGE-547
Code English
ZULRESSO
Brand Name English
Classification Tree Code System Code
FDA ORPHAN DRUG 426114
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
FDA ORPHAN DRUG 399013
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
Code System Code Type Description
INN
10446
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
FDA UNII
S39XZ5QV8Y
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
DRUG CENTRAL
5324
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
NCI_THESAURUS
C169815
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
RXCUI
2121777
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
MERCK INDEX
M1537
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY Merck Index
WIKIPEDIA
ALLOPREGNANOLONE
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
DRUG BANK
DB11859
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
CAS
516-54-1
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
LACTMED
Brexanolone
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
PUBCHEM
92786
Created by admin on Sat Jun 26 16:06:17 UTC 2021 , Edited by admin on Sat Jun 26 16:06:17 UTC 2021
PRIMARY
Related Record Type Details
EXCRETED UNCHANGED
Following administration of radiolabeled brexanolone, 47% was recovered in feces (primarily as metabolites) and 42% in urine (with less than 1% as unchanged brexanolone).
URINE
METABOLIC ENZYME -> SUBSTRATE
BINDER->LIGAND
Plasma protein binding was greater than 99% and is independent of plasma concentrations.
BINDING
TARGET -> ACTIVATOR
MODULATOR
ALLOSTERIC
METABOLIC ENZYME -> SUBSTRATE
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC