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pitolisant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| histamine H3 receptor antagonists, inverse agonists | 5048 | 362665-56-3 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Pitolisant is a potent, orally active histamine H3-receptor antagonist/inverse agonist which, via its blockade of histamine auto-receptors enhances the activity of brain histaminergic neurons, a major arousal system with widespread projections to the whole brain. Pitolisant also modulates various neurotransmitter systems, increasing acetylcholine, noradrenaline and dopamine release in the brain.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 18 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 66 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 1 | Bocci G, Oprea TI, Benet LZ |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,AKT1,AKT2,AKT3,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK4,CDK5,CDK9,CHEK1,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK12,MAPK7,MAPK9,MAPKAPK2,MARK4,MET,MTOR,NTRK2,PAK4,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK | 50 | |||
| kinase-selectivity-class | AKT3,AXL,BRAF,EIF2AK3,EPHB4,GRK2,MAPK7,PDK4,PRKCD,SIK2,STK33,TTK | 12 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 14, 2019 | FDA | HARMONY | |
| March 31, 2016 | EMA | Bioprojet Pharma |
FDA Adverse Event Reporting System (Female)
| 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 |
|---|---|---|---|---|---|---|
| Product administration interrupted | 327.10 | 31.56 | 73 | 2179 | 12419 | 90613776 |
| Surgery | 115.54 | 31.56 | 43 | 2209 | 44844 | 90581351 |
| Anxiety | 95.35 | 31.56 | 71 | 2181 | 309701 | 90316494 |
| Splenic infarction | 87.08 | 31.56 | 18 | 2234 | 2109 | 90624086 |
| Suicidal ideation | 70.27 | 31.56 | 35 | 2217 | 73820 | 90552375 |
| Intentional dose omission | 56.78 | 31.56 | 20 | 2232 | 17763 | 90608432 |
| Cataplexy | 51.48 | 31.56 | 11 | 2241 | 1509 | 90624686 |
| Pre-existing condition improved | 48.08 | 31.56 | 15 | 2237 | 9154 | 90617041 |
| Illness | 37.34 | 31.56 | 24 | 2228 | 81945 | 90544250 |
| Somnambulism | 36.08 | 31.56 | 11 | 2241 | 6217 | 90619978 |
| Depression | 34.83 | 31.56 | 40 | 2212 | 300561 | 90325634 |
| Enuresis | 33.08 | 31.56 | 9 | 2243 | 3405 | 90622790 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Product administration interrupted | 141.25 | 42.74 | 28 | 557 | 4938 | 42615812 |
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Product administration interrupted | 256.81 | 30.11 | 54 | 1652 | 11238 | 110576355 |
| Splenic infarction | 82.72 | 30.11 | 18 | 1688 | 4356 | 110583237 |
| Surgery | 78.79 | 30.11 | 28 | 1678 | 41255 | 110546338 |
| Intentional dose omission | 59.62 | 30.11 | 19 | 1687 | 20061 | 110567532 |
| Anxiety | 50.48 | 30.11 | 42 | 1664 | 345036 | 110242557 |
| Suicidal ideation | 47.81 | 30.11 | 25 | 1681 | 93912 | 110493681 |
| Somnambulism | 36.30 | 30.11 | 10 | 1696 | 6395 | 110581198 |
| Pre-existing condition improved | 36.11 | 30.11 | 10 | 1696 | 6516 | 110581077 |
| Cataplexy | 34.76 | 30.11 | 7 | 1699 | 1162 | 110586431 |
| Sleep apnoea syndrome | 33.38 | 30.11 | 15 | 1691 | 40432 | 110547161 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | N07XX11 | NERVOUS SYSTEM OTHER NERVOUS SYSTEM DRUGS OTHER NERVOUS SYSTEM DRUGS Other nervous system drugs |
| FDA MoA | N0000181003 | Histamine H3 Receptor Antagonists |
| FDA MoA | N0000185506 | Cytochrome P450 3A4 Inducers |
| FDA MoA | N0000194051 | Histamine H3 Receptor Inverse Agonists |
| FDA EPC | N0000194053 | Histamine-3 Receptor Antagonist/Inverse Agonist |
| CHEBI has role | CHEBI:35476 | antipsychotic agent |
| CHEBI has role | CHEBI:48407 | antiparkinson drug |
| CHEBI has role | CHEBI:231911 | renoprotective agent |
Related Drugs by ATC class:
N07XX Other nervous system drugs 23 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Narcolepsy | indication | 60380001 | DOID:8986 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.59 | Basic |
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 17.8MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | 8354430 | Feb. 6, 2026 | METHOD OF TREATING CATAPLEXY IN PATIENTS WITH NARCOLEPSY |
| EQ 17.8MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | 8354430 | Feb. 6, 2026 | METHOD OF TREATING EXCESSIVE DAYTIME SLEEPINESS IN PATIENTS WITH NARCOLEPSY |
| EQ 4.45MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | 8354430 | Feb. 6, 2026 | METHOD OF TREATING CATAPLEXY IN PATIENTS WITH NARCOLEPSY |
| EQ 4.45MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | 8354430 | Feb. 6, 2026 | METHOD OF TREATING EXCESSIVE DAYTIME SLEEPINESS IN PATIENTS WITH NARCOLEPSY |
| EQ 17.8MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | 8486947 | Sept. 26, 2029 | METHOD OF TREATING CATAPLEXY IN PATIENTS WITH NARCOLEPSY |
| EQ 17.8MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | 8486947 | Sept. 26, 2029 | METHOD OF TREATING EXCESSIVE DAYTIME SLEEPINESS IN PATIENTS WITH NARCOLEPSY |
| EQ 4.45MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | 8486947 | Sept. 26, 2029 | METHOD OF TREATING CATAPLEXY IN PATIENTS WITH NARCOLEPSY |
| EQ 4.45MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | 8486947 | Sept. 26, 2029 | METHOD OF TREATING EXCESSIVE DAYTIME SLEEPINESS IN PATIENTS WITH NARCOLEPSY |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 17.8MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | Aug. 14, 2026 | INDICATED FOR THE TREATMENT OF EXCESSIVE DAYTIME SLEEPINESS (EDS) IN ADULT PATIENTS WITH NARCOLEPSY |
| EQ 4.45MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | Aug. 14, 2026 | INDICATED FOR THE TREATMENT OF EXCESSIVE DAYTIME SLEEPINESS (EDS) IN ADULT PATIENTS WITH NARCOLEPSY |
| EQ 17.8MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | June 21, 2027 | NEW PATIENT POPULATION |
| EQ 4.45MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | June 21, 2027 | NEW PATIENT POPULATION |
| EQ 17.8MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | Oct. 13, 2027 | TREATMENT OF CATAPLEXY IN ADULT PATIENTS WITH NACROLEPSY |
| EQ 4.45MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | Oct. 13, 2027 | TREATMENT OF CATAPLEXY IN ADULT PATIENTS WITH NACROLEPSY |
| EQ 17.8MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | June 21, 2031 | TREATMENT OF EXCESSIVE DAYTIME SLEEPINESS (EDS) IN PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH NARCOLEPSY |
| EQ 4.45MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | June 21, 2031 | TREATMENT OF EXCESSIVE DAYTIME SLEEPINESS (EDS) IN PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH NARCOLEPSY |
| EQ 17.8MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | Feb. 13, 2033 | TREATMENT OF CATAPLEXY IN PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH NARCOLEPSY |
| EQ 4.45MG BASE | WAKIX | HARMONY | N211150 | Aug. 14, 2019 | RX | TABLET | ORAL | Feb. 13, 2033 | TREATMENT OF CATAPLEXY IN PEDIATRIC PATIENTS 6 YEARS OF AGE AND OLDER WITH NARCOLEPSY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Histamine H3 receptor | GPCR | INVERSE AGONIST | Ki | 9.80 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Potassium voltage-gated channel subfamily H member 2 | Ion channel | IC50 | 5.77 | CHEMBL | |||||
| Sodium-dependent noradrenaline transporter | Transporter | Ki | 5.72 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 2C | GPCR | Ki | 5.70 | CHEMBL | |||||
| 5-hydroxytryptamine receptor 7 | GPCR | Ki | 5.96 | CHEMBL | |||||
| Histamine H1 receptor | GPCR | Ki | 5.94 | CHEMBL | |||||
| Histamine H2 receptor | GPCR | ANTAGONIST | Ki | 4.96 | IUPHAR | ||||
| Muscarinic acetylcholine receptor M4 | GPCR | Ki | 6.05 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane receptor | Ki | 9.04 | CHEMBL | |||||
| Transmembrane protein 97 | Enzyme | Ki | 8.15 | CHEMBL | |||||
| Sigma non-opioid intracellular receptor 1 | Membrane other | Ki | 9.30 | CHEMBL | |||||
| Cholinesterase | Enzyme | IC50 | 5.08 | CHEMBL | |||||
| Histamine H3 receptor | GPCR | Ki | 7.85 | CHEMBL | |||||
| Histamine H3 receptor | GPCR | Ki | 9.80 | CHEMBL | |||||
| Sigma intracellular receptor 2 | Membrane receptor | Ki | 8.19 | CHEMBL | |||||
| Histamine H3 receptor | GPCR | Ki | 7.77 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4BC83L4PIY | UNII |
| 903576-44-3 | SECONDARY_CAS_RN |
| 4038743 | VANDF |
| 4038744 | VANDF |
| C3529928 | UMLSCUI |
| CHEBI:134709 | CHEBI |
| CHEMBL462605 | ChEMBL_ID |
| 9948102 | PUBCHEM_CID |
| DB11642 | DRUGBANK_ID |
| CHEMBL4164059 | ChEMBL_ID |
| 8952 | INN_ID |
| C516975 | MESH_SUPPLEMENTAL_RECORD_UI |
| 8924 | IUPHAR_LIGAND_ID |
| 2197878 | RXNORM |
| 247019 | MMSL |
| 32128 | MMSL |
| d08498 | MMSL |
| 017799 | NDDF |
| 017884 | NDDF |
| 421000220103 | SNOMEDCT_US |
| 716308007 | SNOMEDCT_US |
| 789360005 | SNOMEDCT_US |
| 4BC83L4PIY | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Wakix | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72028-045 | TABLET, FILM COATED | 4.45 mg | ORAL | NDA | 29 sections |
| Wakix | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72028-045 | TABLET, FILM COATED | 4.45 mg | ORAL | NDA | 29 sections |
| Wakix | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72028-178 | TABLET, FILM COATED | 17.80 mg | ORAL | NDA | 29 sections |
| Wakix | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72028-178 | TABLET, FILM COATED | 17.80 mg | ORAL | NDA | 29 sections |