Stem definition | Drug id | CAS RN |
---|---|---|
1808 | 92623-85-3 |
Dose | Unit | Route |
---|---|---|
0.10 | g | O |
Property | Value | Reference |
---|---|---|
BDDCS (Biopharmaceutical Drug Disposition Classification System) | 3 | Benet LZ, Broccatelli F, Oprea TI |
EoM (Fraction excreted unchanged in urine) | 55 % | Benet LZ, Broccatelli F, Oprea TI |
MRTD (Maximum Recommended Therapeutic Daily Dose) | 11.60 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
BA (Bioavailability) | 84 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Vd (Volume of distribution) | 4.51 L/kg | Lombardo F, Berellini G, Obach RS |
CL (Clearance) | 8.17 mL/min/kg | Lombardo F, Berellini G, Obach RS |
fu (Fraction unbound in plasma) | 0.87 % | Lombardo F, Berellini G, Obach RS |
t_half (Half-life) | 6.48 hours | Lombardo F, Berellini G, Obach RS |
Date | Agency | Company | Orphan |
---|---|---|---|
Jan. 14, 2009 | FDA | CYPRESS BIOSCIENCE |
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 |
---|---|---|---|---|---|---|
Suicidal ideation | 134.84 | 17.59 | 88 | 6677 | 60423 | 53281878 |
Serotonin syndrome | 108.13 | 17.59 | 57 | 6708 | 26349 | 53315952 |
Drug hypersensitivity | 97.03 | 17.59 | 142 | 6623 | 265100 | 53077201 |
Hyperhidrosis | 73.32 | 17.59 | 75 | 6690 | 96718 | 53245583 |
Somatic delusion | 69.36 | 17.59 | 16 | 6749 | 596 | 53341705 |
Nausea | 68.49 | 17.59 | 230 | 6535 | 755861 | 52586440 |
Hot flush | 60.18 | 17.59 | 49 | 6716 | 47111 | 53295190 |
Headache | 50.77 | 17.59 | 166 | 6599 | 536655 | 52805646 |
Depression | 47.52 | 17.59 | 84 | 6681 | 182968 | 53159333 |
Heart rate increased | 45.33 | 17.59 | 54 | 6711 | 82261 | 53260040 |
Urine odour abnormal | 41.09 | 17.59 | 18 | 6747 | 5528 | 53336773 |
Insomnia | 39.99 | 17.59 | 79 | 6686 | 186993 | 53155308 |
Persistent genital arousal disorder | 39.69 | 17.59 | 9 | 6756 | 310 | 53341991 |
Abnormal faeces | 37.81 | 17.59 | 16 | 6749 | 4518 | 53337783 |
Blood pressure increased | 37.12 | 17.59 | 65 | 6700 | 140414 | 53201887 |
Gastrointestinal motility disorder | 36.63 | 17.59 | 16 | 6749 | 4880 | 53337421 |
Blood thyroid stimulating hormone normal | 34.66 | 17.59 | 7 | 6758 | 137 | 53342164 |
Anger | 32.48 | 17.59 | 20 | 6745 | 12370 | 53329931 |
Migraine | 32.09 | 17.59 | 45 | 6720 | 80372 | 53261929 |
Chromaturia | 30.19 | 17.59 | 21 | 6744 | 15929 | 53326372 |
Oral discomfort | 27.83 | 17.59 | 16 | 6749 | 8730 | 53333571 |
Tremor | 26.71 | 17.59 | 53 | 6712 | 125683 | 53216618 |
Lip swelling | 26.04 | 17.59 | 24 | 6741 | 27177 | 53315124 |
Musculoskeletal discomfort | 25.92 | 17.59 | 19 | 6746 | 15641 | 53326660 |
Homicidal ideation | 24.24 | 17.59 | 9 | 6756 | 1805 | 53340496 |
Palpitations | 24.01 | 17.59 | 45 | 6720 | 102303 | 53239998 |
Crying | 23.99 | 17.59 | 21 | 6744 | 22241 | 53320060 |
Aphasia | 23.53 | 17.59 | 24 | 6741 | 30754 | 53311547 |
Flushing | 23.10 | 17.59 | 36 | 6729 | 70564 | 53271737 |
Irritability | 21.62 | 17.59 | 23 | 6742 | 30930 | 53311371 |
Feeling abnormal | 19.65 | 17.59 | 49 | 6716 | 135252 | 53207049 |
Fibromyalgia | 19.59 | 17.59 | 26 | 6739 | 44049 | 53298252 |
Ear infection | 19.44 | 17.59 | 20 | 6745 | 25880 | 53316421 |
Drug withdrawal syndrome | 18.13 | 17.59 | 20 | 6745 | 28002 | 53314299 |
Suicide attempt | 18.11 | 17.59 | 29 | 6736 | 58139 | 53284162 |
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 |
---|---|---|---|---|---|---|
Urinary retention | 55.64 | 26.79 | 26 | 1059 | 35671 | 32476770 |
Suicidal ideation | 48.03 | 26.79 | 24 | 1061 | 38059 | 32474382 |
Agoraphobia | 39.59 | 26.79 | 7 | 1078 | 264 | 32512177 |
Dysuria | 32.20 | 26.79 | 16 | 1069 | 24994 | 32487447 |
Urinary hesitation | 29.14 | 26.79 | 8 | 1077 | 2333 | 32510108 |
Neurosis | 29.07 | 26.79 | 5 | 1080 | 160 | 32512281 |
Source | Code | Description |
---|---|---|
ATC | N06AX17 | NERVOUS SYSTEM PSYCHOANALEPTICS ANTIDEPRESSANTS Other antidepressants |
FDA MoA | N0000000102 | Norepinephrine Uptake Inhibitors |
FDA MoA | N0000000109 | Serotonin Uptake Inhibitors |
MeSH PA | D000700 | Analgesics |
MeSH PA | D018712 | Analgesics, Non-Narcotic |
MeSH PA | D002491 | Central Nervous System Agents |
MeSH PA | D049990 | Membrane Transport Modulators |
MeSH PA | D018377 | Neurotransmitter Agents |
MeSH PA | D014179 | Neurotransmitter Uptake Inhibitors |
MeSH PA | D018373 | Peripheral Nervous System Agents |
MeSH PA | D018689 | Sensory System Agents |
MeSH PA | D000068760 | Serotonin and Noradrenaline Reuptake Inhibitors |
FDA EPC | N0000175749 | Serotonin and Norepinephrine Reuptake Inhibitor |
Disease | Relation | SNOMED_ID | DOID |
---|---|---|---|
Fibromyalgia | indication | 203082005 | DOID:631 |
Tachyarrhythmia | contraindication | 6285003 | |
Urinary tract obstruction | contraindication | 7163005 | DOID:5200 |
Alcoholism | contraindication | 7200002 | |
Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
Disorder of cardiovascular system | contraindication | 49601007 | DOID:1287 |
Syndrome of inappropriate vasopressin secretion | contraindication | 55004003 | DOID:3401 |
Acute nephropathy | contraindication | 58574008 | |
Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
Hyponatremia | contraindication | 89627008 | |
Seizure disorder | contraindication | 128613002 | |
Liver function tests abnormal | contraindication | 166603001 | |
Mania | contraindication | 231494001 | |
Hypomania | contraindication | 231496004 | |
Disease of liver | contraindication | 235856003 | DOID:409 |
Suicidal | contraindication | 267073005 | |
Serotonin syndrome | contraindication | 371089000 | |
Angle-closure glaucoma | contraindication | 392291006 | DOID:13550 |
Dissociation level | Dissociation constant | Type (acidic/basic) |
---|---|---|
pKa1 | 10.64 | Basic |
Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
---|---|---|---|---|---|---|---|---|---|---|
100MG | SAVELLA | ALLERGAN | N022256 | Jan. 14, 2009 | RX | TABLET | ORAL | 6602911 | Jan. 14, 2023 | MANAGEMENT OF FIBROMYALGIA (FM) |
12.5MG | SAVELLA | ALLERGAN | N022256 | Jan. 14, 2009 | RX | TABLET | ORAL | 6602911 | Jan. 14, 2023 | MANAGEMENT OF FIBROMYALGIA (FM) |
25MG | SAVELLA | ALLERGAN | N022256 | Jan. 14, 2009 | RX | TABLET | ORAL | 6602911 | Jan. 14, 2023 | MANAGEMENT OF FIBROMYALGIA (FM) |
50MG | SAVELLA | ALLERGAN | N022256 | Jan. 14, 2009 | RX | TABLET | ORAL | 6602911 | Jan. 14, 2023 | MANAGEMENT OF FIBROMYALGIA (FM) |
100MG | SAVELLA | ALLERGAN | N022256 | Jan. 14, 2009 | RX | TABLET | ORAL | 7994220 | Sept. 19, 2029 | MANAGEMENT OF FIBROMYALGIA |
12.5MG | SAVELLA | ALLERGAN | N022256 | Jan. 14, 2009 | RX | TABLET | ORAL | 7994220 | Sept. 19, 2029 | MANAGEMENT OF FIBROMYALGIA |
25MG | SAVELLA | ALLERGAN | N022256 | Jan. 14, 2009 | RX | TABLET | ORAL | 7994220 | Sept. 19, 2029 | MANAGEMENT OF FIBROMYALGIA |
50MG | SAVELLA | ALLERGAN | N022256 | Jan. 14, 2009 | RX | TABLET | ORAL | 7994220 | Sept. 19, 2029 | MANAGEMENT OF FIBROMYALGIA |
None
Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
---|---|---|---|---|---|---|---|---|---|
Sodium-dependent serotonin transporter | Transporter | INHIBITOR | Ki | 7.29 | WOMBAT-PK | CHEMBL | |||
Sodium-dependent noradrenaline transporter | Transporter | INHIBITOR | Ki | 7.60 | WOMBAT-PK | CHEMBL | |||
Sodium-dependent dopamine transporter | Transporter | IC50 | 5.21 | CHEMBL | |||||
Glutamate receptor ionotropic, NMDA 2A | Ion channel | IC50 | 5.20 | WOMBAT-PK | |||||
Sodium-dependent serotonin transporter | Transporter | IC50 | 7.33 | CHEMBL | |||||
Sodium-dependent dopamine transporter | Transporter | IC50 | 4.43 | CHEMBL | |||||
Transporter | Transporter | IC50 | 7.52 | CHEMBL |
ID | Source |
---|---|
4025253 | VUID |
N0000179785 | NUI |
D01107 | KEGG_DRUG |
101152-94-7 | SECONDARY_CAS_RN |
4025253 | VANDF |
4028372 | VANDF |
C1533126 | UMLSCUI |
CHEBI:135005 | CHEBI |
CHEMBL252923 | ChEMBL_ID |
CHEMBL259209 | ChEMBL_ID |
DB04896 | DRUGBANK_ID |
CHEMBL4297064 | ChEMBL_ID |
D000078764 | MESH_DESCRIPTOR_UI |
5701 | INN_ID |
65833 | PUBCHEM_CID |
7436 | IUPHAR_LIGAND_ID |
G56VK1HF36 | UNII |
30003 | RXNORM |
26139 | MMSL |
d06635 | MMSL |
008263 | NDDF |
008264 | NDDF |
441641002 | SNOMEDCT_US |
442542004 | SNOMEDCT_US |
442642007 | SNOMEDCT_US |
CHEMBL1237129 | ChEMBL_ID |
Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
---|---|---|---|---|---|---|---|---|
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0456-1510 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 37 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0456-1512 | TABLET, FILM COATED | 12.50 mg | ORAL | NDA | 37 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0456-1525 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 37 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0456-1550 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 37 sections |
SAVELLA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-845 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 35 sections |
SAVELLA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-846 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 35 sections |
SAVELLA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 16590-847 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 35 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-650 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 34 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 21695-651 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 34 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 35356-545 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 33 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50436-9993 | TABLET, FILM COATED | 25 mg | ORAL | NDA | 33 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6024 | TABLET, FILM COATED | 100 mg | ORAL | NDA | 33 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-6043 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 33 sections |
Savella | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55154-4626 | TABLET, FILM COATED | 50 mg | ORAL | NDA | 33 sections |
Milnacipran HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-091 | TABLET | 12.50 mg | ORAL | ANDA | 20 sections |
Milnacipran HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-092 | TABLET | 25 mg | ORAL | ANDA | 20 sections |
Milnacipran HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-093 | TABLET | 50 mg | ORAL | ANDA | 20 sections |
Milnacipran HCl | HUMAN PRESCRIPTION DRUG LABEL | 1 | 65162-094 | TABLET | 100 mg | ORAL | ANDA | 20 sections |