Lumateperone

Lumateperone
Clinical data
Pronunciation/ˌlməˈtɛpərn/
LOO-mə-TE-pər-ohn
Trade namesCaplyta
Other namesITI-007; ITI-722
AHFS/Drugs.comMonograph
MedlinePlusa620014
License data
Routes of
administration
By mouth
Drug classAtypical antipsychotic
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability4.4%[1]
Protein binding97.4%[1]
MetabolismMultiple UGTs, CYP450s, and AKR enzymes[1]
Excretion<1% excreted unchanged in urine[1]
Identifiers
IUPAC name
  • 1-(4-Fluorophenyl)-4-(3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)-1-butanone
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC24H28FN3O
Molar mass393.506 g·mol−1
3D model (JSmol)
SMILES
  • CN1CCN2c3c(cccc31)[C@@H]1CN(CCCC(=O)c3ccc(F)cc3)CC[C@@H]12
InChI
  • InChI=1S/C24H28FN3O/c1-26-14-15-28-21-11-13-27(16-20(21)19-4-2-5-22(26)24(19)28)12-3-6-23(29)17-7-9-18(25)10-8-17/h2,4-5,7-10,20-21H,3,6,11-16H2,1H3/t20-,21-/m0/s1
  • Key:HOIIHACBCFLJET-SFTDATJTSA-N

Lumateperone, sold under the brand name Caplyta, is an atypical antipsychotic medication of the pyridopyrroloquinoxaline and butyrophenone families. It is approved for the treatment of schizophrenia as well as bipolar depression, as either monotherapy or adjunctive therapy (with lithium or valproate).[1] It is developed by Intra-Cellular Therapies, licensed from Bristol-Myers Squibb.[2] Lumateperone was approved for medical use in the United States in December 2019 with an initial indication for schizophrenia,[3][4] and became available in February 2020.[1] It has since demonstrated efficacy in bipolar depression and received FDA approval in December 2021 for depressive episodes associated with both bipolar I and II disorders. Part of the drug shows structural similarity to Pirlindole.

  1. ^ a b c d e f g Cite error: The named reference Caplyta FDA label was invoked but never defined (see the help page).
  2. ^ Celanire S, Poli S, eds. (13 October 2014). Small Molecule Therapeutics for Schizophrenia. Springer. pp. 31–. ISBN 978-3-319-11502-3.
  3. ^ Cite error: The named reference FDA snapshot was invoked but never defined (see the help page).
  4. ^ Cite error: The named reference FDA approval was invoked but never defined (see the help page).