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1. Acp 103
2. Acp-103
3. Acp103
4. Bis(1-(4-fluorobenzyl)-1-(1-methylpiperidin-4-yl)-3-(4-(2-methylpropoxy)benzyl)urea) (2r,3r)-2,3-dihydroxybutanedioate
5. N-(4-fluorophenylmethyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide
6. Nuplazid
7. Pimavanserin Tartrate
8. Urea, N-((4-fluorophenyl)methyl)-n-(1-methyl-4-piperidinyl)-n'-((4-(2-methylpropoxy)phenyl)methyl)-, (2r,3r)-2,3-dihydroxybutanedioate (2:1)
1. 706779-91-1
2. Acp-103
3. 1-(4-fluorobenzyl)-3-(4-isobutoxybenzyl)-1-(1-methylpiperidin-4-yl)urea
4. Pimavanserin [inn]
5. Pimavanserin Free Base
6. Jz963p0dik
7. 706779-91-1 (free Base)
8. 1-[(4-fluorophenyl)methyl]-1-(1-methylpiperidin-4-yl)-3-[[4-(2-methylpropoxy)phenyl]methyl]urea
9. N-(4-fluorophenylmethyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl) Carbamide
10. Unii-jz963p0dik
11. N-(4-fluorophenylmethyl)-n-(1-methylpiperidin-4-yl)-n'-(4-(2-methylpropyloxy)phenylmethyl)carbamide
12. 706782-28-7
13. Pimanavserin
14. Methyltrimethylacetate
15. Ac-5273
16. Pimavanserin [mi]
17. Pimavanserin(acp-103)
18. Pimavanserin [who-dd]
19. Schembl675165
20. Nuplazid (proposed Trade Name)
21. Gtpl8423
22. Chembl2111101
23. Dtxsid90990906
24. Chebi:133017
25. Bdbm139370
26. Hms3742a03
27. Bcp11618
28. Ex-a4895
29. Mfcd09953792
30. Zinc16159083
31. Akos015902593
32. Cs-3378
33. Db05316
34. Me-0240
35. Sb16963
36. Ncgc00390656-01
37. Ncgc00390656-02
38. Hy-14557
39. B8019
40. Ft-0653701
41. A14434
42. 779p911
43. A836958
44. J-503297
45. Q7194603
46. N-[(4-fluorophenyl)methyl]-n-(1-methyl-4-piperidinyl)-n'-[[4-(2-methylpropoxy)phenyl]methyl]urea;
47. N-[(4-fluorophenyl)methyl]-n-(1-methylpiperidin-4-yl)-n'-{[4-(2-methylpropoxy)phenyl]methyl}urea
Molecular Weight | 427.6 g/mol |
---|---|
Molecular Formula | C25H34FN3O2 |
XLogP3 | 4.5 |
Hydrogen Bond Donor Count | 1 |
Hydrogen Bond Acceptor Count | 4 |
Rotatable Bond Count | 8 |
Exact Mass | 427.26350550 g/mol |
Monoisotopic Mass | 427.26350550 g/mol |
Topological Polar Surface Area | 44.8 Ų |
Heavy Atom Count | 31 |
Formal Charge | 0 |
Complexity | 523 |
Isotope Atom Count | 0 |
Defined Atom Stereocenter Count | 0 |
Undefined Atom Stereocenter Count | 0 |
Defined Bond Stereocenter Count | 0 |
Undefined Bond Stereocenter Count | 0 |
Covalently Bonded Unit Count | 1 |
Pimavanserin is indicated for the treatment of hallucinations and delusions associated with Parkinsons disease psychosis.
Treatment of schizophrenia and other psychotic disorders
Pimavanserin's unique actions on serotonin receptors improve symptoms of hallucinations and delusions associated with Parkinson's disease. In clinical studies, 80.5% of individuals treated with pimavanserin reported improvement in symptoms. Pimavanserin does not worsen motor functioning in patients with Parkinson's disease psychosis.
Antiparkinson Agents
Agents used in the treatment of Parkinson's disease. The most commonly used drugs act on the dopaminergic system in the striatum and basal ganglia or are centrally acting muscarinic antagonists. (See all compounds classified as Antiparkinson Agents.)
Antipsychotic Agents
Agents that control agitated psychotic behavior, alleviate acute psychotic states, reduce psychotic symptoms, and exert a quieting effect. They are used in SCHIZOPHRENIA; senile dementia; transient psychosis following surgery; or MYOCARDIAL INFARCTION; etc. These drugs are often referred to as neuroleptics alluding to the tendency to produce neurological side effects, but not all antipsychotics are likely to produce such effects. Many of these drugs may also be effective against nausea, emesis, and pruritus. (See all compounds classified as Antipsychotic Agents.)
Serotonin 5-HT2 Receptor Antagonists
Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes. (See all compounds classified as Serotonin 5-HT2 Receptor Antagonists.)
N - Nervous system
N05 - Psycholeptics
N05A - Antipsychotics
N05AX - Other antipsychotics
N05AX17 - Pimavanserin
Absorption
The median Tmax of pimavanserin in clinical studies was 6 hours, regardless of the dose. Bioavailability of an oral tablet of pimavanserin and a solution were almost identical. The major active circulating N-desmethylated metabolite, AC-279, has a median Tmax of 6 hours.
Route of Elimination
About 0.55% of a 34 mg oral dose was excreted unchanged in the urine and 1.53% was eliminated in feces within 10 days. Less than 1% of the administered dose and its active metabolite AC-279 were recovered in urine during clinical studies.
Volume of Distribution
Following administration of a single dose of 34 mg, the average apparent volume of distribution was 2173 L in clinical studies.
Pimavanserin is mainly metabolized CYP3A4 and CYP3A5 hepatic cytochrome enzymes, and to a lesser extent by CYP2J2, CYP2D6, and other cytochrome and flavin-containing monooxygenase enzymes. CYP3A4 metabolizes pimavanserin to its major active metabolite, AC-279.
The average plasma half-lives for pimavanserin and its active metabolite (AC-279) are estimated at 57 hours and 200 hours, respectively.
Parkinson's disease psychosis (PDP) is a imbalance of serotonin and dopamine from disruption of the normal balance between the serotonergic and dopaminergic receptors and neurotransmitters in the brain. The mechanism by which pimavanserin treats hallucinations and delusions associated with Parkinsons disease psychosis is not fully established. It is possible that pimavanserin acts via inverse agonist and antagonist activity at serotonin 5-HT2A receptors with limited effects on serotonin 5-HT2C receptors. Pimavanserin is an inverse agonist and antagonist of serotonin 5-HT2A receptors with high binding affinity, demonstrating low binding affinity to serotonin 5-HT2C receptors. In addition, this drug exhibits low affinity binding to sigma 1 receptors. Pimavanserin lacks activity at muscarinic, dopaminergic, adrenergic, and histaminergic receptors, preventing various undesirable effects typically associated with antipsychotics.
API Imports and Exports
Importing Country | Total Quantity (KGS) |
Average Price (USD/KGS) |
Number of Transactions |
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Details:
Nuplazid (pimavanserin) is an atypical antipsychotic 5-HT2A receptor inverse agonist, which is being evaluated for the treatment of patients with schizophrenia.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Psychiatry/Psychology Product Name: Nuplazid
Highest Development Status: Phase IIIProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable March 11, 2024
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Psychiatry/Psychology
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Details : Nuplazid (pimavanserin) is an atypical antipsychotic 5-HT2A receptor inverse agonist, which is being evaluated for the treatment of patients with schizophrenia.
Product Name : Nuplazid
Product Type : Small molecule
Upfront Cash : Not Applicable
March 11, 2024
Details:
Nuplazid (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, which is used treatment for Parkinson’s disease-related hallucinations and delusions who also have dementia.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Neurology Product Name: Nuplazid
Highest Development Status: ApprovedProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable September 18, 2023
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Neurology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Acadia Pharmaceuticals Announces Label Update for NUPLAZID® (pimavanserin)
Details : Nuplazid (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, which is used treatment for Parkinson’s disease-related hallucinations and delusions ...
Product Name : Nuplazid
Product Type : Small molecule
Upfront Cash : Not Applicable
September 18, 2023
Details:
NUPLAZID (Pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors and prevents psychosis symptoms associated with Parkinson's Disease Psychosis.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Psychiatry/Psychology Product Name: Nuplazid
Highest Development Status: ApprovedProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable January 03, 2023
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Psychiatry/Psychology
Highest Development Status : Approved
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Newly Published Retrospective Analysis Showed Lower All-Cause Mortality Risk Among Parkinson’s D...
Details : NUPLAZID (Pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors and prevents psychosis symptoms associated with Parkinson's Disease Psychosis.
Product Name : Nuplazid
Product Type : Small molecule
Upfront Cash : Not Applicable
January 03, 2023
Details:
Nuplazid (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, demonstrated no appreciable binding affinity for dopamine (including D2), histamine, muscarinic, or adrenergic receptors.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Psychiatry/Psychology Product Name: Nuplazid
Highest Development Status: Phase IIIProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable August 04, 2022
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Psychiatry/Psychology
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
U.S. FDA Declines to Approve Expanded Use of Acadia's Antipsychotic Drug
Details : Nuplazid (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, demonstrated no appreciable binding affinity for dopamine (including D2), histamine, mu...
Product Name : Nuplazid
Product Type : Small molecule
Upfront Cash : Not Applicable
August 04, 2022
Details:
Nuplazid (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, which is used Treatment of Hallucinations and Delusions Associated with Alzheimer’s Disease Psychosis.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Psychiatry/Psychology Product Name: Nuplazid
Highest Development Status: Phase IIIProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable August 04, 2022
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Psychiatry/Psychology
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Details : Nuplazid (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, which is used Treatment of Hallucinations and Delusions Associated with Alzheimer’s D...
Product Name : Nuplazid
Product Type : Small molecule
Upfront Cash : Not Applicable
August 04, 2022
Details:
Nuplazid (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, which is used Treatment of Alzheimer’s Disease Psychosis.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Psychiatry/Psychology Product Name: Nuplazid
Highest Development Status: Phase IIIProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable June 17, 2022
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Psychiatry/Psychology
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Acadia Pharmaceuticals Announces Outcome of FDA Advisory Committee for NUPLAZID® (pimavanserin) f...
Details : Nuplazid (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, which is used Treatment of Alzheimer’s Disease Psychosis.
Product Name : Nuplazid
Product Type : Small molecule
Upfront Cash : Not Applicable
June 17, 2022
Details:
ACP-103 (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, demonstrated no appreciable binding affinity for dopamine, histamine, muscarinic, or adrenergic receptors in vitro.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Psychiatry/Psychology Product Name: Nuplazid
Highest Development Status: Phase IIIProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable May 02, 2022
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Psychiatry/Psychology
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Details : ACP-103 (pimavanserin) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, demonstrated no appreciable binding affinity for dopamine, histamine, muscarinic, or adr...
Product Name : Nuplazid
Product Type : Small molecule
Upfront Cash : Not Applicable
May 02, 2022
Details:
ACP-103 (pimavanserin tartrate) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors for the treatment of hallucinations and delusions associated with Alzheimer’s disease psychosis.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Psychiatry/Psychology Product Name: ACP-103
Highest Development Status: Phase IIIProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable March 09, 2022
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Psychiatry/Psychology
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Details : ACP-103 (pimavanserin tartrate) is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors for the treatment of hallucinations and delusions associated with Alzheimer’s ...
Product Name : ACP-103
Product Type : Small molecule
Upfront Cash : Not Applicable
March 09, 2022
Details:
Resubmission for Nuplazid (pimavanserin) provides additional analyses from two previously conducted clinical studies, HARMONY1 and Study -0192, to support a proposed indication for treatment of ADP and is intended to address issues raised in FDA’s CRL.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Neurology Product Name: Nuplazid
Highest Development Status: Phase IIIProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable February 16, 2022
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Neurology
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Details : Resubmission for Nuplazid (pimavanserin) provides additional analyses from two previously conducted clinical studies, HARMONY1 and Study -0192, to support a proposed indication for treatment of ADP and is inten...
Product Name : Nuplazid
Product Type : Small molecule
Upfront Cash : Not Applicable
February 16, 2022
Details:
Pimavanserin tablet is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, which is used treatment for Parkinson's disease.
Lead Product(s): Pimavanserin Tartrate
Therapeutic Area: Psychiatry/Psychology Product Name: Nuplazid-Generic
Highest Development Status: Phase IIIProduct Type: Small molecule
Partner/Sponsor/Collaborator: Not Applicable
Deal Size: Not Applicable Upfront Cash: Not Applicable
Deal Type: Not Applicable January 27, 2022
Lead Product(s) : Pimavanserin Tartrate
Therapeutic Area : Psychiatry/Psychology
Highest Development Status : Phase III
Partner/Sponsor/Collaborator : Not Applicable
Deal Size : Not Applicable
Deal Type : Not Applicable
Sun Pharma Gets SEC Nod For Phase III Clinical Trial For Antipsychotic Drug Pimavanserin
Details : Pimavanserin tablet is a selective serotonin inverse agonist and antagonist preferentially targeting 5-HT2A receptors, which is used treatment for Parkinson's disease.
Product Name : Nuplazid-Generic
Product Type : Small molecule
Upfront Cash : Not Applicable
January 27, 2022
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