Details of the Drug

General Information of Drug (ID: DMR7IVC)

• Drug Name: Pimavanserin
• Synonyms: ST51054136; AC-5273; I14-1981; 1-[(4-fluorophenyl)methyl]-1-(1-methyl-4-piperidyl)-3-[[4-(2-methylpropoxy)phenyl]methyl]urea

Indication

Disease Entry	ICD 11	Status	REF
Parkinson disease	8A00.0	Approved	[1]

• Drug Type: Small molecular drug
• #Ro5 Violations (Lipinski): 0:
  Molecular Weight (mw); 427.6
  Logarithm of the Partition Coefficient (xlogp); 4.5
  Rotatable Bond Count (rotbonds); 8
  Hydrogen Bond Donor Count (hbonddonor); 1
  Hydrogen Bond Acceptor Count (hbondacc); 4
• ADMET Property:
  Absorption Cmax: The maximum plasma concentration (Cmax) of drug is 4.7 +/- 1.6 mg/L []
  Absorption Tmax: The time to maximum plasma concentration (Tmax) is 131 +/- 56 h []
  Elimination: 0.55% of a 34 mg oral dose was excreted unchanged in the urine and 1.53% was eliminated in feces [2]
  Half-life: The concentration or amount of drug in body reduced by one-half in 57 hours [3]
  Metabolism: The drug is metabolized via the hepatic [3]
  Vd: The volume of distribution (Vd) of drug is 2173 L [2]
• Chemical Identifiers:
  Formula: C25H34FN3O2
  IUPAC Name: 1-[(4-fluorophenyl)methyl]-1-(1-methylpiperidin-4-yl)-3-[[4-(2-methylpropoxy)phenyl]methyl]urea
  Canonical SMILES: CC(C)COC1=CC=C(C=C1)CNC(=O)N(CC2=CC=C(C=C2)F)C3CCN(CC3)C
  InChI: InChI=1S/C25H34FN3O2/c1-19(2)18-31-24-10-6-20(7-11-24)16-27-25(30)29(23-12-14-28(3)15-13-23)17-21-4-8-22(26)9-5-21/h4-11,19,23H,12-18H2,1-3H3,(H,27,30)
  InChIKey: RKEWSXXUOLRFBX-UHFFFAOYSA-N
• Cross-matching ID:
  PubChem CID: 10071196
  ChEBI ID: CHEBI:133017
  CAS Number: 706779-91-1
  DrugBank ID: DB05316
  TTD ID: D0J8JP
  ACDINA ID: D00531

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
5-HT 2A receptor (HTR2A)	TTJQOD7	5HT2A_HUMAN	Modulator	[4]

Molecular Expression Atlas of This Drug

• The Studied Disease: Parkinson disease
• ICD Disease Classification: 8A00.0

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
5-HT 2A receptor (HTR2A)	DTT	HTR2A	1.68E-01	-0.3	-0.14
5-HT 2A receptor (HTR2A)	DTT	HTR2A	5.59E-01	0.15	0.21

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Pimavanserin (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Metreleptin	DM1NOEK	Moderate	Increased metabolism of Pimavanserin caused by Metreleptin mediated induction of CYP450 enzyme.	Acute diabete complication [5A2Y]	[5]
Ivosidenib	DM8S6T7	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Ivosidenib.	Acute myeloid leukaemia [2A60]	[6]
Midostaurin	DMI6E0R	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Midostaurin.	Acute myeloid leukaemia [2A60]	[5]
Arn-509	DMT81LZ	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Arn-509.	Acute myeloid leukaemia [2A60]	[7]
Gilteritinib	DMTI0ZO	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Gilteritinib.	Acute myeloid leukaemia [2A60]	[5]
Oliceridine	DM6MDCF	Major	Additive CNS depression effects by the combination of Pimavanserin and Oliceridine.	Acute pain [MG31]	[8]
Ivabradine	DM0L594	Major	Increased risk of ventricular arrhythmias by the combination of Pimavanserin and Ivabradine.	Angina pectoris [BA40]	[7]
Bedaquiline	DM3906J	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Bedaquiline.	Antimicrobial drug resistance [MG50-MG52]	[9]
Levalbuterol	DM5YBO1	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Levalbuterol.	Asthma [CA23]	[10]
Troleandomycin	DMUZNIG	Major	Decreased metabolism of Pimavanserin caused by Troleandomycin mediated inhibition of CYP450 enzyme.	Bacterial infection [1A00-1C4Z]	[5]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of Pimavanserin caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[5]
Eribulin	DM1DX4Q	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Eribulin.	Breast cancer [2C60-2C6Y]	[5]
Tucatinib	DMBESUA	Major	Decreased metabolism of Pimavanserin caused by Tucatinib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[5]
Palbociclib	DMD7L94	Moderate	Decreased metabolism of Pimavanserin caused by Palbociclib mediated inhibition of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[5]
Bosutinib	DMTI8YE	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Bosutinib.	Breast cancer [2C60-2C6Y]	[5]
PF-04449913	DMSB068	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and PF-04449913.	Chronic myelomonocytic leukaemia [2A40]	[5]
Olodaterol	DM62B78	Moderate	Increased risk of ventricular arrhythmias by the combination of Pimavanserin and Olodaterol.	Chronic obstructive pulmonary disease [CA22]	[11]
Vilanterol	DMF5EK1	Moderate	Increased risk of ventricular arrhythmias by the combination of Pimavanserin and Vilanterol.	Chronic obstructive pulmonary disease [CA22]	[10]
Osilodrostat	DMIJC9X	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Osilodrostat.	Cushing syndrome [5A70]	[5]
Ivacaftor	DMZC1HS	Moderate	Decreased metabolism of Pimavanserin caused by Ivacaftor mediated inhibition of CYP450 enzyme.	Cystic fibrosis [CA25]	[5]
MK-8228	DMOB58Q	Moderate	Decreased metabolism of Pimavanserin caused by MK-8228 mediated inhibition of CYP450 enzyme.	Cytomegaloviral disease [1D82]	[5]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Pimavanserin and Esketamine.	Depression [6A70-6A7Z]	[12]
Deutetrabenazine	DMUPFLI	Moderate	Additive CNS depression effects by the combination of Pimavanserin and Deutetrabenazine.	Dystonic disorder [8A02]	[13]
Ingrezza	DMVPLNC	Moderate	Additive CNS depression effects by the combination of Pimavanserin and Ingrezza.	Dystonic disorder [8A02]	[14]
Cenobamate	DM8KLU9	Moderate	Increased metabolism of Pimavanserin caused by Cenobamate mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[5]
Stiripentol	DMMSDOY	Moderate	Decreased metabolism of Pimavanserin caused by Stiripentol mediated inhibition of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[5]
Rufinamide	DMWE60C	Moderate	Increased metabolism of Pimavanserin caused by Rufinamide mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[5]
Eslicarbazepine	DMZREFQ	Moderate	Increased metabolism of Pimavanserin caused by Eslicarbazepine mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[5]
Boceprevir	DMBSHMF	Major	Decreased metabolism of Pimavanserin caused by Boceprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[5]
Telaprevir	DMMRV29	Major	Decreased metabolism of Pimavanserin caused by Telaprevir mediated inhibition of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[5]
MK-1439	DM215WE	Moderate	Increased metabolism of Pimavanserin caused by MK-1439 mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[5]
Fostemsavir	DM50ILT	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Fostemsavir.	Human immunodeficiency virus disease [1C60-1C62]	[5]
Cobicistat	DM6L4H2	Major	Decreased metabolism of Pimavanserin caused by Cobicistat mediated inhibition of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[5]
Etravirine	DMGV8QU	Moderate	Increased metabolism of Pimavanserin caused by Etravirine mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[5]
Rilpivirine	DMJ0QOW	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Rilpivirine.	Human immunodeficiency virus disease [1C60-1C62]	[5]
BMS-201038	DMQTAGO	Moderate	Decreased metabolism of Pimavanserin caused by BMS-201038 mediated inhibition of CYP450 enzyme.	Hyper-lipoproteinaemia [5C80]	[5]
Lesinurad	DMUR64T	Moderate	Increased metabolism of Pimavanserin caused by Lesinurad mediated induction of CYP450 enzyme.	Inborn purine/pyrimidine/nucleotide metabolism error [5C55]	[5]
Suvorexant	DM0E6S3	Moderate	Decreased metabolism of Pimavanserin caused by Suvorexant mediated inhibition of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[5]
Polyethylene glycol	DM4I1JP	Moderate	Increased risk of ventricular arrhythmias by the combination of Pimavanserin and Polyethylene glycol.	Irritable bowel syndrome [DD91]	[7]
Glycerol phenylbutyrate	DMDGRQO	Moderate	Increased metabolism of Pimavanserin caused by Glycerol phenylbutyrate mediated induction of CYP450 enzyme.	Liver disease [DB90-DB9Z]	[5]
Crizotinib	DM4F29C	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Crizotinib.	Lung cancer [2C25]	[15]
Brigatinib	DM7W94S	Moderate	Increased metabolism of Pimavanserin caused by Brigatinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[5]
Ceritinib	DMB920Z	Major	Decreased metabolism of Pimavanserin caused by Ceritinib mediated inhibition of CYP450 enzyme.	Lung cancer [2C25]	[5]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of Pimavanserin caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[5]
Osimertinib	DMRJLAT	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Osimertinib.	Lung cancer [2C25]	[16]
Selpercatinib	DMZR15V	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Selpercatinib.	Lung cancer [2C25]	[7]
Lumefantrine	DM29GAD	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Lumefantrine.	Malaria [1F40-1F45]	[12]
Inotuzumab ozogamicin	DMAC130	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Inotuzumab ozogamicin.	Malignant haematopoietic neoplasm [2B33]	[5]
Idelalisib	DM602WT	Major	Decreased metabolism of Pimavanserin caused by Idelalisib mediated inhibition of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[5]
Vemurafenib	DM62UG5	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Vemurafenib.	Melanoma [2C30]	[17]
LGX818	DMNQXV8	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and LGX818.	Melanoma [2C30]	[5]
Dabrafenib	DMX6OE3	Moderate	Increased metabolism of Pimavanserin caused by Dabrafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[5]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Pimavanserin and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[18]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Pimavanserin and Lasmiditan.	Migraine [8A80]	[19]
Siponimod	DM2R86O	Major	Increased risk of ventricular arrhythmias by the combination of Pimavanserin and Siponimod.	Multiple sclerosis [8A40]	[12]
Ozanimod	DMT6AM2	Major	Increased risk of ventricular arrhythmias by the combination of Pimavanserin and Ozanimod.	Multiple sclerosis [8A40]	[20]
Romidepsin	DMT5GNL	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Romidepsin.	Mycosis fungoides [2B01]	[5]
Entrectinib	DMMPTLH	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Entrectinib.	Non-small cell lung cancer [2C25]	[12]
Rucaparib	DM9PVX8	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Rucaparib.	Ovarian cancer [2C73]	[5]
Triclabendazole	DMPWGBR	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Triclabendazole.	Parasitic worm infestation [1F90]	[5]
Macimorelin	DMQYJIR	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Macimorelin.	Pituitary gland disorder [5A60-5A61]	[21]
Lefamulin	DME6G97	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Lefamulin.	Pneumonia [CA40]	[22]
Lonafarnib	DMGM2Z6	Major	Decreased metabolism of Pimavanserin caused by Lonafarnib mediated inhibition of CYP450 enzyme.	Premature ageing appearance [LD2B]	[5]
Degarelix	DM3O8QY	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Degarelix.	Prostate cancer [2C82]	[7]
ABIRATERONE	DM8V75C	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and ABIRATERONE.	Prostate cancer [2C82]	[7]
Enzalutamide	DMGL19D	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Enzalutamide.	Prostate cancer [2C82]	[7]
Relugolix	DMK7IWL	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Relugolix.	Prostate cancer [2C82]	[7]
Amisulpride	DMSJVAM	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Amisulpride.	Schizophrenia [6A20]	[23]
Asenapine	DMSQZE2	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Asenapine.	Schizophrenia [6A20]	[17]
Voxelotor	DMCS6M5	Moderate	Decreased metabolism of Pimavanserin caused by Voxelotor mediated inhibition of CYP450 enzyme.	Sickle-cell disorder [3A51]	[5]
Telotristat ethyl	DMDIYFZ	Moderate	Increased metabolism of Pimavanserin caused by Telotristat ethyl mediated induction of CYP450 enzyme.	Small intestine developmental anomaly [DA90]	[5]
Larotrectinib	DM26CQR	Moderate	Decreased metabolism of Pimavanserin caused by Larotrectinib mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[5]
Armodafinil	DMGB035	Moderate	Increased metabolism of Pimavanserin caused by Armodafinil mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[5]
LEE011	DMMX75K	Moderate	Decreased metabolism of Pimavanserin caused by LEE011 mediated inhibition of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[5]
Triptorelin	DMTK4LS	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Triptorelin.	Solid tumour/cancer [2A00-2F9Z]	[7]
Pitolisant	DM8RFNJ	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Pitolisant.	Somnolence [MG42]	[5]
Telavancin	DM58VQX	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Telavancin.	Staphylococcal/streptococcal disease [1B5Y]	[5]
Brilinta	DMBR01X	Moderate	Decreased metabolism of Pimavanserin caused by Brilinta mediated inhibition of CYP450 enzyme.	Thrombosis [DB61-GB90]	[5]
Lenvatinib	DMB1IU4	Moderate	Increased risk of prolong QT interval by the combination of Pimavanserin and Lenvatinib.	Thyroid cancer [2D10]	[5]
Cabozantinib	DMIYDT4	Major	Increased risk of prolong QT interval by the combination of Pimavanserin and Cabozantinib.	Thyroid cancer [2D10]	[7]
Elagolix	DMB2C0E	Moderate	Increased metabolism of Pimavanserin caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[5]

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
FD&C blue no. 1	E00263	19700	Colorant
Saccharin sodium anhydrous	E00443	656582	Flavoring agent
Ferric oxide black	E00522	16211978	Colorant
Hypromellose	E00634	Not Available	Coating agent
Magnesium stearate	E00208	11177	lubricant
Polyethylene glycol 3350	E00652	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyethylene glycol 4000	E00654	Not Available	Coating agent; Diluent; Ointment base; Plasticizing agent; Solvent; Suppository base; lubricant
Polyvinyl alcohol	E00666	Not Available	Coating agent; Emulsion stabilizing agent; Film/Membrane-forming agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
Colcothar yellow	E00436	518696	Colorant
Haematite red	E00236	14833	Colorant
Cellulose microcrystalline	E00698	Not Available	Adsorbent; Suspending agent; Diluent
Pregelatinized starch	E00674	Not Available	Binding agent; Diluent; Disintegrant

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Pimavanserin 17 mg tablet	17 mg	Oral Tablet	Oral
Pimavanserin Tartrate 10 mg tablet	10 mg	Tablet	Oral
Pimavanserin Tartrate 34 mg capsule	34 mg	Capsule	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

• [1] 2016 FDA drug approvals. Nat Rev Drug Discov. 2017 Feb 2;16(2):73-76.
• [2] Cruz MP: Pimavanserin (Nuplazid): A Treatment for Hallucinations and Delusions Associated With Parkinson's Disease. P T. 2017 Jun;42(6):368-371.
• [3] FDA Approved Drug Product: NUPLAZID (pimavanserin) for oral use
• [4] Pimavanserin, a selective serotonin (5-HT)2A-inverse agonist, enhances the efficacy and safety of risperidone, 2mg/day, but does not enhance efficacy of haloperidol, 2mg/day: comparison with reference dose risperidone, 6mg/day.Schizophr Res.2012 Nov;141(2-3):144-52.
• [5] Product Information. Nuplazid (pimavanserin). Accelis Pharma, East Windsor, NJ.
• [6] Product Information. Tibsovo (ivosidenib). Agios Pharmaceuticals, Cambridge, MA.
• [7] Cerner Multum, Inc. "UK Summary of Product Characteristics.".
• [8] US Food and Drug Administration "FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines requires its strongest warning.".
• [9] Product Information. Sirturo (bedaquiline). Janssen Pharmaceuticals, Titusville, NJ.
• [10] Product Information. Arcapta Neohaler (indacaterol). Novartis Pharmaceuticals, East Hanover, NJ.
• [11] Bengtsson B, Fagerstrom PO "Extrapulmonary effects of terbutaline during prolonged administration." Clin Pharmacol Ther 31 (1982): 726-32. [PMID: 7042176]
• [12] Cerner Multum, Inc. "Australian Product Information.".
• [13] Product Information. Austedo (deutetrabenazine). Teva Pharmaceuticals USA, North Wales, PA.
• [14] Product Information. Ingrezza (valbenazine). Neurocrine Biosciences, Inc., San Diego, CA.
• [15] Product Information. Xalkori (crizotinib). Pfizer U.S. Pharmaceuticals Group, New York, NY.
• [16] Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
• [17] Canadian Pharmacists Association.
• [18] Product Information. Zulresso (brexanolone). Sage Therapeutics, Inc., Cambridge, MA.
• [19] Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
• [20] Product Information. Zeposia (ozanimod). Celgene Corporation, Summit, NJ.
• [21] Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
• [22] Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
• [23] Product Information. Barhemsys (amisulpride). Acacia Pharma, Inc, Indianapolis, IN.