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Brexpiprazole

These highlights do not include all the information needed to use BREXPIPRAZOLE TABLETS safely and effectively. See full prescribing information for BREXPIPRAZOLE TABLETS. BREXPIPRAZOLE tablets, for oral use Initial U.S. Approval: 2015

Approved
Approval ID

993b584c-7fe6-4551-899f-39146c8508ac

Product Type

HUMAN PRESCRIPTION DRUG LABEL

Effective Date

Dec 13, 2022

Manufacturers
FDA

Ajanta Pharma USA Inc.

DUNS: 557554156

Products 6

Detailed information about drug products covered under this FDA approval, including NDC codes, dosage forms, ingredients, and administration routes.

Brexpiprazole

Product Details

FDA regulatory identification and product classification information

FDA Identifiers
NDC Product Code27241-207
Application NumberANDA213718
Product Classification
M
Marketing Category
C73584
G
Generic Name
Brexpiprazole
Product Specifications
Route of AdministrationORAL
Effective DateDecember 13, 2022
FDA Product Classification

INGREDIENTS (11)

MICROCRYSTALLINE CELLULOSEInactive
Code: OP1R32D61U
Classification: IACT
HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 9XZ8H6N6OH
Classification: IACT
BREXPIPRAZOLEActive
Quantity: 2 mg in 1 1
Code: 2J3YBM1K8C
Classification: ACTIB
LACTOSE MONOHYDRATEInactive
Code: EWQ57Q8I5X
Classification: IACT
HYPROMELLOSE, UNSPECIFIEDInactive
Code: 3NXW29V3WO
Classification: IACT
TITANIUM DIOXIDEInactive
Code: 15FIX9V2JP
Classification: IACT
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 2165RE0K14
Classification: IACT
MAGNESIUM STEARATEInactive
Code: 70097M6I30
Classification: IACT
POLYETHYLENE GLYCOL, UNSPECIFIEDInactive
Code: 3WJQ0SDW1A
Classification: IACT
FD&C BLUE NO. 2Inactive
Code: L06K8R7DQK
Classification: IACT
FERRIC OXIDE YELLOWInactive
Code: EX438O2MRT
Classification: IACT

Brexpiprazole

Product Details

FDA regulatory identification and product classification information

FDA Identifiers
NDC Product Code27241-209
Application NumberANDA213718
Product Classification
M
Marketing Category
C73584
G
Generic Name
Brexpiprazole
Product Specifications
Route of AdministrationORAL
Effective DateDecember 13, 2022
FDA Product Classification

INGREDIENTS (9)

BREXPIPRAZOLEActive
Quantity: 4 mg in 1 1
Code: 2J3YBM1K8C
Classification: ACTIB
LACTOSE MONOHYDRATEInactive
Code: EWQ57Q8I5X
Classification: IACT
MICROCRYSTALLINE CELLULOSEInactive
Code: OP1R32D61U
Classification: IACT
HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 9XZ8H6N6OH
Classification: IACT
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 2165RE0K14
Classification: IACT
MAGNESIUM STEARATEInactive
Code: 70097M6I30
Classification: IACT
TITANIUM DIOXIDEInactive
Code: 15FIX9V2JP
Classification: IACT
HYPROMELLOSE, UNSPECIFIEDInactive
Code: 3NXW29V3WO
Classification: IACT
POLYETHYLENE GLYCOL, UNSPECIFIEDInactive
Code: 3WJQ0SDW1A
Classification: IACT

Brexpiprazole

Product Details

FDA regulatory identification and product classification information

FDA Identifiers
NDC Product Code27241-204
Application NumberANDA213718
Product Classification
M
Marketing Category
C73584
G
Generic Name
Brexpiprazole
Product Specifications
Route of AdministrationORAL
Effective DateDecember 13, 2022
FDA Product Classification

INGREDIENTS (11)

BREXPIPRAZOLEActive
Quantity: 0.25 mg in 1 1
Code: 2J3YBM1K8C
Classification: ACTIB
LACTOSE MONOHYDRATEInactive
Code: EWQ57Q8I5X
Classification: IACT
MICROCRYSTALLINE CELLULOSEInactive
Code: OP1R32D61U
Classification: IACT
HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 9XZ8H6N6OH
Classification: IACT
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 2165RE0K14
Classification: IACT
MAGNESIUM STEARATEInactive
Code: 70097M6I30
Classification: IACT
TALCInactive
Code: 7SEV7J4R1U
Classification: IACT
PROPYLENE GLYCOLInactive
Code: 6DC9Q167V3
Classification: IACT
FERRIC OXIDE REDInactive
Code: 1K09F3G675
Classification: IACT
HYPROMELLOSE, UNSPECIFIEDInactive
Code: 3NXW29V3WO
Classification: IACT
TITANIUM DIOXIDEInactive
Code: 15FIX9V2JP
Classification: IACT

Brexpiprazole

Product Details

FDA regulatory identification and product classification information

FDA Identifiers
NDC Product Code27241-205
Application NumberANDA213718
Product Classification
M
Marketing Category
C73584
G
Generic Name
Brexpiprazole
Product Specifications
Route of AdministrationORAL
Effective DateDecember 13, 2022
FDA Product Classification

INGREDIENTS (11)

MICROCRYSTALLINE CELLULOSEInactive
Code: OP1R32D61U
Classification: IACT
BREXPIPRAZOLEActive
Quantity: 0.5 mg in 1 1
Code: 2J3YBM1K8C
Classification: ACTIB
HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 9XZ8H6N6OH
Classification: IACT
LACTOSE MONOHYDRATEInactive
Code: EWQ57Q8I5X
Classification: IACT
HYPROMELLOSE, UNSPECIFIEDInactive
Code: 3NXW29V3WO
Classification: IACT
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 2165RE0K14
Classification: IACT
MAGNESIUM STEARATEInactive
Code: 70097M6I30
Classification: IACT
TALCInactive
Code: 7SEV7J4R1U
Classification: IACT
TITANIUM DIOXIDEInactive
Code: 15FIX9V2JP
Classification: IACT
PROPYLENE GLYCOLInactive
Code: 6DC9Q167V3
Classification: IACT
FD&C YELLOW NO. 6Inactive
Code: H77VEI93A8
Classification: IACT

Brexpiprazole

Product Details

FDA regulatory identification and product classification information

FDA Identifiers
NDC Product Code27241-206
Application NumberANDA213718
Product Classification
M
Marketing Category
C73584
G
Generic Name
Brexpiprazole
Product Specifications
Route of AdministrationORAL
Effective DateDecember 13, 2022
FDA Product Classification

INGREDIENTS (11)

LACTOSE MONOHYDRATEInactive
Code: EWQ57Q8I5X
Classification: IACT
BREXPIPRAZOLEActive
Quantity: 1 mg in 1 1
Code: 2J3YBM1K8C
Classification: ACTIB
HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 9XZ8H6N6OH
Classification: IACT
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 2165RE0K14
Classification: IACT
MICROCRYSTALLINE CELLULOSEInactive
Code: OP1R32D61U
Classification: IACT
TALCInactive
Code: 7SEV7J4R1U
Classification: IACT
HYPROMELLOSE, UNSPECIFIEDInactive
Code: 3NXW29V3WO
Classification: IACT
MAGNESIUM STEARATEInactive
Code: 70097M6I30
Classification: IACT
TITANIUM DIOXIDEInactive
Code: 15FIX9V2JP
Classification: IACT
FERRIC OXIDE YELLOWInactive
Code: EX438O2MRT
Classification: IACT
PROPYLENE GLYCOLInactive
Code: 6DC9Q167V3
Classification: IACT

Brexpiprazole

Product Details

FDA regulatory identification and product classification information

FDA Identifiers
NDC Product Code27241-208
Application NumberANDA213718
Product Classification
M
Marketing Category
C73584
G
Generic Name
Brexpiprazole
Product Specifications
Route of AdministrationORAL
Effective DateDecember 13, 2022
FDA Product Classification

INGREDIENTS (11)

BREXPIPRAZOLEActive
Quantity: 3 mg in 1 1
Code: 2J3YBM1K8C
Classification: ACTIB
MICROCRYSTALLINE CELLULOSEInactive
Code: OP1R32D61U
Classification: IACT
HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 9XZ8H6N6OH
Classification: IACT
LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE, UNSPECIFIEDInactive
Code: 2165RE0K14
Classification: IACT
MAGNESIUM STEARATEInactive
Code: 70097M6I30
Classification: IACT
TITANIUM DIOXIDEInactive
Code: 15FIX9V2JP
Classification: IACT
FERRIC OXIDE REDInactive
Code: 1K09F3G675
Classification: IACT
LACTOSE MONOHYDRATEInactive
Code: EWQ57Q8I5X
Classification: IACT
HYPROMELLOSE, UNSPECIFIEDInactive
Code: 3NXW29V3WO
Classification: IACT
POLYETHYLENE GLYCOL, UNSPECIFIEDInactive
Code: 3WJQ0SDW1A
Classification: IACT
FERRIC OXIDE YELLOWInactive
Code: EX438O2MRT
Classification: IACT

Drug Labeling Information

RECENT MAJOR CHANGES SECTION

LOINC: 43683-2Updated: 12/13/2022

RECENT MAJOR CHANGES

Boxed Warning 12/2021
Warnings and Precautions (5.6) 12/2021

USE IN SPECIFIC POPULATIONS SECTION

LOINC: 43684-0Updated: 12/13/2022

8 USE IN SPECIFIC POPULATIONS

8.1 Pregnancy

Pregnancy Exposure Registry

There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to brexpiprazole tablets during pregnancy. For more information contact the National Pregnancy Registry for Atypical Antipsychotics at 1-866-961-2388 or visit http://womensmentalhealth.org/clinical-and-research- programs/pregnancyregistry/.

Risk Summary

Adequate and well-controlled studies have not been conducted with brexpiprazole tablets in pregnant women to inform drug-associated risks. However, neonates whose mothers are exposed to antipsychotic drugs, like brexpiprazole tablets, during the third trimester of pregnancy are at risk for extrapyramidal and/or withdrawal symptoms. In animal reproduction studies, no teratogenicity was observed with oral administration of brexpiprazole to pregnant rats and rabbits during organogenesis at doses up to 73 and 146 times, respectively, of maximum recommended human dose (MRHD) of 4 mg/day on a mg/m2 basis. However, when pregnant rats were administered brexpiprazole during the period of organogenesis through lactation, the number of perinatal deaths of pups was increased at 73 times the MRHD [see Data]. The background risk of major birth defects and miscarriage for the indicated population(s) is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Clinical Considerations

Fetal/Neonatal Adverse Reactions

Extrapyramidal and/or withdrawal symptoms, including agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress and feeding disorder, have been reported in neonates whose mothers were exposed to antipsychotic drugs during the third trimester of pregnancy. These symptoms have varied in severity. Some neonates recovered within hours or days without specific treatment; others required prolonged hospitalization. Monitor neonates for extrapyramidal and/or withdrawal symptoms and manage symptoms appropriately.

Data

Animal Data

Pregnant rats were treated with oral doses of 3 mg/kg/day, 10 mg/kg/day, and 30 mg/kg/day (7.3, 24, and 73 times the MRHD on a mg/m2 basis) of brexpiprazole during the period of organogenesis. Brexpiprazole was not teratogenic and did not cause adverse developmental effects at doses up to 73 times the MRHD.

Pregnant rabbits were treated with oral doses of 10 mg/kg/day, 30 mg/kg/day, and 150 mg/kg/day (49, 146, and 730 times the MRHD) of brexpiprazole during the period of organogenesis. Brexpiprazole was not teratogenic and did not cause adverse developmental effects at doses up to 146 times the MRHD. Findings of decreased body weight, retarded ossification, and increased incidences of visceral and skeletal variations were observed in fetuses at 730 times the MRHD, a dose that induced maternal toxicity.

In a study in which pregnant rats were administered oral doses of 3 mg/kg/day, 10 mg/kg/day, and 30 mg/kg/day (7.3, 24, and 73 times the MRHD) during the period of organogenesis and through lactation, the number of live-born pups was decreased, and early postnatal deaths increased at a dose 73 times the MRHD. Impaired nursing by dams, and low birth weight and decreased body weight gain in pups were observed at 73 times, but not at 24 times, the MRHD.

8.2 Lactation

Risk Summary

Lactation studies have not been conducted to assess the presence of brexpiprazole in human milk, the effects of brexpiprazole on the breastfed infant, or the effects of brexpiprazole on milk production. Brexpiprazole is present in rat milk. The development and health benefits of breastfeeding should be considered along with the mother’s clinical need for brexpiprazole tablets and any potential adverse effects on the breastfed infant from brexpiprazole tablets or from the underlying maternal condition.

8.4 Pediatric Use

Major Depressive Disorder
Safety and effectiveness in pediatric patients with major depressive disorder have not been established. Antidepressants increased the risk of suicidal thoughts and behaviors in pediatric patients [see Boxed Warning, Warnings and Precautions (5.2)].

Pediatric use information is approved for Otsuka Pharmaceutical Company, Ltd.’s Rexulti® (brexpiprazole) tablets. However, due to Otsuka Pharmaceutical Company, LTD.’s marketing exclusivity rights, this drug product is not labeled with that information.

8.5 Geriatric Use

Clinical studies of the efficacy of brexpiprazole tablets did not include any patients aged 65 or older to determine whether they respond differently from younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, and cardiac function, concomitant diseases, and other drug therapy.

Based on the results of a safety, tolerability, and pharmacokinetics trial, the pharmacokinetics of once daily oral administration of brexpiprazole (up to 3 mg/day for 14 days) as an adjunct therapy in the treatment of elderly patients (70 to 85 years old, N=11) with MDD were comparable to those observed in adult patients with MDD.

Antipsychotic drugs increase the risk of death in elderly patients with dementia-related psychosis. Brexpiprazole tablets are not approved for the treatment of patients with dementia-related psychosis [see Boxed Warning, Warnings and Precautions (5.1)].

8.6 CYP2D6 Poor Metabolizers

Dosage adjustment is recommended in known CYP2D6 poor metabolizers, because these patients have higher brexpiprazole concentrations than normal metabolizers of CYP2D6. Approximately 8% of Caucasians and 3% to 8% of Black/African Americans cannot metabolize CYP2D6 substrates and are classified as poor metabolizers [see Dosage and Administration (2.5), Clinical Pharmacology (12.3)].

8.7 Hepatic Impairment

Reduce the maximum recommended dosage in patients with moderate to severe hepatic impairment (Child-Pugh score greater than or equal to 7). Patients with moderate to severe hepatic impairment (Child-Pugh score greater than or equal to 7) generally had higher exposure to brexpiprazole than patients with normal hepatic function [see Clinical Pharmacology (12.3)]. Greater exposure may increase the risk of brexpiprazole tablets-associated adverse reactions [see Dosage and Administration (2.3)].

8.8 Renal Impairment

Reduce the maximum recommended dosage in patients with moderate, severe, or end-stage renal impairment (CrCl less than 60 mL/minute). Patients with impaired renal function (CrCl less than 60 mL/minute) had higher exposure to brexpiprazole than patients with normal renal function [see Clinical Pharmacology (12.3)]. Greater exposure may increase the risk of brexpiprazole tablets-associated adverse reactions [see Dosage and Administration (2.4)].

8.9 Other Specific Populations

No dosage adjustment for brexpiprazole tablets is required on the basis of a patient’s sex, race, or smoking status [see Clinical Pharmacology (12.3)].

Key Highlight

Pregnancy: May cause extrapyramidal and/or withdrawal symptoms in neonates with third trimester exposure (8.1)

Pediatric use information is approved for Otsuka Pharmaceutical Company, Ltd.’s Rexulti® (brexpiprazole) tablets. However, due to Otsuka Pharmaceutical Company, Ltd.’s marketing exclusivity rights, this drug product is not labeled with that information.

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