Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C21H34O2 |
Molecular Weight | 318.4935 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 8 / 8 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@@]12CC[C@H](C(C)=O)[C@@]1(C)CC[C@@]3([H])[C@@]2([H])CC[C@@]4([H])C[C@H](O)CC[C@]34C
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
Molecular Formula | C21H34O2 |
Molecular Weight | 318.4935 |
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
Doses
Dose | Population | Adverse 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... Other AEs: Dizziness (grade 1, 13%) 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: |
Other AEs: Diarrhea, Dry mouth... Other AEs: Diarrhea (3%) Sources: Dry mouth (11%) Oropharyngeal pain (3%) Loss of consciousness (5%) Flush hot (5%) |
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 AEs leading toSyncope Somnolence Dizziness Fatigue Infusion related reaction Change in blood pressure discontinuation/dose reduction: Loss of consciousness Sources: Vertigo Syncope Presyncope Infusion site pain |
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%) Sources: Diarrhea (2%) Dry mouth (3%) Dyspepsia (2%) Oropharyngeal pain (2%) Dizziness (12%) Loss of consciousness (3%) Somnolence (13%) 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, 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%) Sources: 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%) |
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%) Sources: Feeling of relaxation (9.4%) Feeling abnormal (6.3%) Psychomotor retardation (3.1%) Euphoric mood (12.5%) |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
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: |
Overview
CYP3A4 | CYP2C9 | CYP2D6 | hERG |
---|---|---|---|
OverviewOther
Other Inhibitor | Other Substrate | Other Inducer |
---|---|---|
Drug as perpetrator
Target | Modality | Activity | Metabolite | Clinical 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
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
unlikely | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes | ||||
yes |
Tox targets
Target | Modality | Activity | Metabolite | Clinical evidence |
---|---|---|---|---|
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT02603926
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
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24012744
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
Edited
Sat Dec 16 08:10:21 GMT 2023
by
admin
on
Sat Dec 16 08:10:21 GMT 2023
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Record UNII |
S39XZ5QV8Y
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Record Status |
Validated (UNII)
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Record Version |
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-
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Classification Tree | Code System | Code | ||
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FDA ORPHAN DRUG |
426114
Created by
admin on Sat Dec 16 08:10:21 GMT 2023 , Edited by admin on Sat Dec 16 08:10:21 GMT 2023
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FDA ORPHAN DRUG |
399013
Created by
admin on Sat Dec 16 08:10:21 GMT 2023 , Edited by admin on Sat Dec 16 08:10:21 GMT 2023
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Code System | Code | Type | Description | ||
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10446
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S39XZ5QV8Y
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5324
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PRIMARY | |||
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C169815
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50169
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DE-17
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PRIMARY | |||
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2121777
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m1537
Created by
admin on Sat Dec 16 08:10:21 GMT 2023 , Edited by admin on Sat Dec 16 08:10:21 GMT 2023
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PRIMARY | Merck Index | ||
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100000177178
Created by
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DTXSID901016239
Created by
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S39XZ5QV8Y
Created by
admin on Sat Dec 16 08:10:21 GMT 2023 , Edited by admin on Sat Dec 16 08:10:21 GMT 2023
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ALLOPREGNANOLONE
Created by
admin on Sat Dec 16 08:10:21 GMT 2023 , Edited by admin on Sat Dec 16 08:10:21 GMT 2023
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DB11859
Created by
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516-54-1
Created by
admin on Sat Dec 16 08:10:21 GMT 2023 , Edited by admin on Sat Dec 16 08:10:21 GMT 2023
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PRIMARY | |||
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Brexanolone
Created by
admin on Sat Dec 16 08:10:21 GMT 2023 , Edited by admin on Sat Dec 16 08:10:21 GMT 2023
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PRIMARY | |||
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92786
Created by
admin on Sat Dec 16 08:10:21 GMT 2023 , Edited by admin on Sat Dec 16 08:10:21 GMT 2023
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PRIMARY |
Related Record | Type | Details | ||
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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
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METABOLIC ENZYME -> SUBSTRATE | |||
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TARGET -> ACTIVATOR |
MODULATOR
ALLOSTERIC
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BINDER->LIGAND |
Plasma protein binding was greater than 99% and is independent of plasma concentrations.
BINDING
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METABOLIC ENZYME -> SUBSTRATE |
Related Record | Type | Details | ||
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METABOLITE -> PARENT | |||
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METABOLITE -> PARENT |
Related Record | Type | Details | ||
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Volume of Distribution | PHARMACOKINETIC |
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Biological Half-life | PHARMACOKINETIC |
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