Stem definition | Drug id | CAS RN |
---|---|---|
psychotropics, phenylpiperazine derivatives | 5014 | 913611-97-9 |
Dose | Unit | Route |
---|---|---|
3 | mg | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Hosey CM, Chan R, Benet LZ |
Vd (Volume of distribution) | 1.46 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 0.34 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.00 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 54.37 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
July 27, 2018 | EMA | OTSUKA PHARM CO LTD | |
Jan. 19, 2018 | PMDA | Otsuka Pharmaceutical Co., Ltd. | |
July 10, 2015 | FDA | OTSUKA PHARM CO LTD |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Akathisia | 385.15 | 27.86 | 96 | 3846 | 7618 | 46674502 |
Weight increased | 298.61 | 27.86 | 180 | 3762 | 164293 | 46517827 |
Off label use | 222.73 | 27.86 | 211 | 3731 | 379630 | 46302490 |
Restlessness | 106.51 | 27.86 | 49 | 3893 | 25475 | 46656645 |
Tardive dyskinesia | 94.10 | 27.86 | 32 | 3910 | 7511 | 46674609 |
Schizoaffective disorder | 92.36 | 27.86 | 22 | 3920 | 1430 | 46680690 |
Inability to afford medication | 80.97 | 27.86 | 19 | 3923 | 1157 | 46680963 |
Product administered to patient of inappropriate age | 78.85 | 27.86 | 22 | 3920 | 2674 | 46679446 |
Suicidal ideation | 77.37 | 27.86 | 52 | 3890 | 56330 | 46625790 |
Mania | 75.70 | 27.86 | 30 | 3912 | 10816 | 46671304 |
Product use in unapproved indication | 65.62 | 27.86 | 57 | 3885 | 90216 | 46591904 |
Sinus rhythm | 48.16 | 27.86 | 11 | 3931 | 594 | 46681526 |
Anxiety | 47.37 | 27.86 | 67 | 3875 | 181890 | 46500230 |
Anger | 43.97 | 27.86 | 21 | 3921 | 11831 | 46670289 |
Depression | 43.33 | 27.86 | 62 | 3880 | 170042 | 46512078 |
Wrong technique in product usage process | 42.83 | 27.86 | 36 | 3906 | 54386 | 46627734 |
Tremor | 41.64 | 27.86 | 50 | 3892 | 115589 | 46566531 |
Drug level increased | 37.87 | 27.86 | 22 | 3920 | 18419 | 46663701 |
Adverse event | 36.33 | 27.86 | 27 | 3915 | 34157 | 46647963 |
Eye movement disorder | 36.04 | 27.86 | 14 | 3928 | 4779 | 46677341 |
Extrapyramidal disorder | 35.91 | 27.86 | 18 | 3924 | 11250 | 46670870 |
Food craving | 31.59 | 27.86 | 9 | 3933 | 1178 | 46680942 |
Insomnia | 30.62 | 27.86 | 52 | 3890 | 164872 | 46517248 |
Compulsive shopping | 30.32 | 27.86 | 8 | 3934 | 787 | 46681333 |
Feeling abnormal | 29.50 | 27.86 | 44 | 3898 | 125016 | 46557104 |
Sedation | 28.69 | 27.86 | 20 | 3922 | 22890 | 46659230 |
Electrocardiogram QT prolonged | 28.65 | 27.86 | 28 | 3914 | 51297 | 46630823 |
Increased appetite | 28.29 | 27.86 | 14 | 3928 | 8513 | 46673607 |
MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
---|---|---|---|---|---|---|
Akathisia | 223.97 | 36.67 | 54 | 1575 | 5850 | 29944999 |
Off label use | 107.61 | 36.67 | 96 | 1533 | 249194 | 29701655 |
Weight increased | 98.33 | 36.67 | 57 | 1572 | 74856 | 29875993 |
Product administered to patient of inappropriate age | 74.78 | 36.67 | 19 | 1610 | 2524 | 29948325 |
Tardive dyskinesia | 66.13 | 36.67 | 20 | 1609 | 5037 | 29945812 |
Restlessness | 57.85 | 36.67 | 27 | 1602 | 22572 | 29928277 |
Suicidal ideation | 51.27 | 36.67 | 29 | 1600 | 36085 | 29914764 |
Anxiety | 49.36 | 36.67 | 40 | 1589 | 89831 | 29861018 |
No adverse event | 48.28 | 36.67 | 22 | 1607 | 17397 | 29933452 |
Schizophrenia | 40.27 | 36.67 | 16 | 1613 | 9032 | 29941817 |
Inability to afford medication | 39.23 | 36.67 | 9 | 1620 | 776 | 29950073 |
Apathy | 38.49 | 36.67 | 14 | 1615 | 6218 | 29944631 |
Source | Code | Description |
---|---|---|
ATC | N05AX16 | NERVOUS SYSTEM PSYCHOLEPTICS ANTIPSYCHOTICS Other antipsychotics |
FDA EPC | N0000175430 | Atypical Antipsychotic |
MeSH PA | D015259 | Dopamine Agents |
MeSH PA | D018491 | Dopamine Agonists |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D018490 | Serotonin Agents |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Schizophrenia | indication | 58214004 | DOID:5419 |
Major depressive disorder | indication | 370143000 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 12.14 | acidic |
pKa2 | 8.07 | Basic |
pKa3 | 0.9 | Basic |
None
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
D(2) dopamine receptor | GPCR | AGONIST | Ki | 9.52 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
5-hydroxytryptamine receptor 1A | GPCR | AGONIST | Ki | 9.92 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
5-hydroxytryptamine receptor 2A | GPCR | ANTAGONIST | Ki | 9.33 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
5-hydroxytryptamine receptor 2C | GPCR | Ki | 7.47 | SCIENTIFIC LITERATURE | |||||
5-hydroxytryptamine receptor 5A | GPCR | Ki | 6.85 | SCIENTIFIC LITERATURE | |||||
5-hydroxytryptamine receptor 6 | GPCR | Ki | 7.24 | SCIENTIFIC LITERATURE | |||||
Alpha-1A adrenergic receptor | GPCR | Ki | 8.42 | SCIENTIFIC LITERATURE | |||||
Alpha-2A adrenergic receptor | GPCR | Ki | 7.82 | SCIENTIFIC LITERATURE | |||||
Alpha-2B adrenergic receptor | GPCR | Ki | 7.77 | SCIENTIFIC LITERATURE | |||||
Beta-1 adrenergic receptor | GPCR | Ki | 7.23 | SCIENTIFIC LITERATURE | |||||
Beta-2 adrenergic receptor | GPCR | Ki | 7.17 | SCIENTIFIC LITERATURE | |||||
Sodium-dependent serotonin transporter | Transporter | INHIBITOR | IC50 | 7.54 | SCIENTIFIC LITERATURE | ||||
Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | IC50 | 6.86 | SCIENTIFIC LITERATURE | ||||
Sodium-dependent dopamine transporter | Transporter | INHIBITOR | IC50 | 6.02 | SCIENTIFIC LITERATURE | ||||
D(3) dopamine receptor | GPCR | AGONIST | Ki | 8.96 | SCIENTIFIC LITERATURE | ||||
5-hydroxytryptamine receptor 2B | GPCR | ANTAGONIST | Ki | 8.72 | SCIENTIFIC LITERATURE | ||||
Alpha-1B adrenergic receptor | GPCR | ANTAGONIST | Ki | 9.77 | SCIENTIFIC LITERATURE | ||||
Alpha-2C adrenergic receptor | GPCR | ANTAGONIST | Ki | 9.23 | SCIENTIFIC LITERATURE | ||||
Histamine H1 receptor | GPCR | ANTAGONIST | Ki | 7.72 | SCIENTIFIC LITERATURE | ||||
5-hydroxytryptamine receptor 7 | GPCR | ANTAGONIST | Ki | 8.43 | SCIENTIFIC LITERATURE | ||||
D(1A) dopamine receptor | GPCR | AGONIST | Ki | 6.80 | SCIENTIFIC LITERATURE | ||||
Alpha-1D adrenergic receptor | GPCR | ANTAGONIST | Ki | 8.59 | SCIENTIFIC LITERATURE | ||||
D(4) dopamine receptor | GPCR | AGONIST | Ki | 8.20 | SCIENTIFIC LITERATURE | ||||
5-hydroxytryptamine receptor 1B | GPCR | Ki | 7.49 | SCIENTIFIC LITERATURE |
ID | Source |
---|---|
2J3YBM1K8C | UNII |
D10309 | KEGG_DRUG |
4034625 | VUID |
N0000191737 | NUI |
4034625 | VANDF |
C3885614 | UMLSCUI |
CHEBI:134716 | CHEBI |
CHEMBL2105760 | ChEMBL_ID |
DB09128 | DRUGBANK_ID |
9552 | INN_ID |
C000591922 | MESH_SUPPLEMENTAL_RECORD_UI |
11978813 | PUBCHEM_CID |
7672 | IUPHAR_LIGAND_ID |
1658314 | RXNORM |
234913 | MMSL |
31120 | MMSL |
d08373 | MMSL |
016270 | NDDF |
716069007 | SNOMEDCT_US |
781292006 | SNOMEDCT_US |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Rexulti | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59148-035 | TABLET | 0.25 mg | ORAL | NDA | 37 sections |
Rexulti | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59148-036 | TABLET | 0.50 mg | ORAL | NDA | 37 sections |
Rexulti | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59148-037 | TABLET | 1 mg | ORAL | NDA | 37 sections |
Rexulti | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59148-038 | TABLET | 2 mg | ORAL | NDA | 37 sections |
Rexulti | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59148-039 | TABLET | 3 mg | ORAL | NDA | 37 sections |
Rexulti | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59148-040 | TABLET | 4 mg | ORAL | NDA | 37 sections |