tezacaftor 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
cystic fibrosis transmembrane regulator (CFTR) protein modulators, correctors, and amplifiers	5276	1152311-62-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: tezacaftor VX-661	Tezacaftor facilitates the cellular processing and trafficking of normal and select mutant forms of CFTR (including F508del-CFTR) to increase the amount of mature CFTR protein delivered to the cell surface. Molecular weight: 520.51 Formula: C26H27F3N2O6 CLOGP: 2.78 LIPINSKI: 1 HAC: 8 HDO: 4 TPSA: 113.18 ALOGS: -4.62 ROTB: 8 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

tezacaftor
VX-661

Tezacaftor facilitates the cellular processing and trafficking of normal and select mutant forms of CFTR (including F508del-CFTR) to increase the amount of mature CFTR protein delivered to the cell surface.

Molecular weight: 520.51
Formula: C26H27F3N2O6
CLOGP: 2.78
LIPINSKI: 1
HAC: 8
HDO: 4
TPSA: 113.18
ALOGS: -4.62
ROTB: 8

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ

Approvals:

Date	Agency	Company	Orphan
Aug. 21, 2020	EMA	Vertex Pharmaceuticals (Ireland) Limited
Feb. 12, 2018	FDA	VERTEX PHARMS

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R07AX31	RESPIRATORY SYSTEM OTHER RESPIRATORY SYSTEM PRODUCTS OTHER RESPIRATORY SYSTEM PRODUCTS Other respiratory system products
ATC	R07AX32	RESPIRATORY SYSTEM OTHER RESPIRATORY SYSTEM PRODUCTS OTHER RESPIRATORY SYSTEM PRODUCTS Other respiratory system products

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Drug Use | Suggest Off label Use Form| |View source of the data|

Disease	Relation	SNOMED_ID	DOID
Cystic fibrosis of the lung	indication	86555001

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.64	acidic
pKa2	13.25	acidic
pKa3	13.99	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	8629162	June 24, 2025	TEZACAFTOR AND IVACAFTOR FOR THE TREATMENT OF PATIENTS WITH A MILD TO MODERATE CLINICAL PHENOTYPE OF CYSTIC FIBROSIS HAVING AT LEAST ONE CFTR GENE MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR BASED ON IN VITRO DATA AND/OR CLINICAL EVIDENCE
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	8354427	July 6, 2026	TEZACAFTOR AND IVACAFTOR FOR THE TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGE 6 YEARS AND OLDER WHO HAVE A R117H MUTATION IN THE CFTR GENE
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	9670163	Dec. 28, 2026	TEZACAFTOR AND IVACAFTOR FOR THE TREATMENT OF CYSTIC FIBROSIS IN PATIENTS WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR HAVING AT LEAST ONE CFTR GENE MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR BASED ON IN VITRO DATA AND/OR CLINICAL EVIDENCE
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	9931334	Dec. 28, 2026	TREATING CYSTIC FIBROSIS PATIENTS AGES 12 AND OLDER, WHO ARE HOMOZYGOUS FOR F508DEL OR HAVE AT LEAST 1 CFTR GENE MUTATION RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH TEZACAFTOR AND A SOLID COMPOSITION COMPRISING AMORPHOUS (<30% CRYSTALLINE) IVACAFTOR
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	9931334	Dec. 28, 2026	TREATING CYSTIC FIBROSIS PATIENTS AGES 6 AND OLDER, WHO ARE HOMOZYGOUS FOR F508DEL OR HAVE AT LEAST 1 CFTR GENE MUTATION RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH TEZACAFTOR AND A SOLID COMPOSITION COMPRISING AMORPHOUS (<30% CRYSTALLINE) IVACAFTOR
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	10022352	April 9, 2027	TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 12 YEARS AND OLDER, WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR HETEROZYGOUS FOR F508DEL AND A SECOND CFTR MUTATION PREDICTED TO BE RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH TEZACAFTOR AND IVACAFTOR
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	10022352	April 9, 2027	TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 6 YEARS AND OLDER, WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR HETEROZYGOUS FOR F508DEL AND A SECOND CFTR MUTATION PREDICTED TO BE RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH TEZACAFTOR AND IVACAFTOR
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	10239867	April 9, 2027	TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 12 YEARS AND OLDER, WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR HAVE AT LEAST ONE CFTR MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH AN EFFECTIVE AMOUNT OF TEZACAFTOR AND IVACAFTOR
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	10239867	April 9, 2027	TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 6 YEARS AND OLDER, WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR HAVE AT LEAST ONE CFTR MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH AN EFFECTIVE AMOUNT OF TEZACAFTOR AND IVACAFTOR
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	11639347	April 9, 2027	TREATMENT OF CYSTIC FIBROSIS IN PATIENTS AGED 6 YEARS AND OLDER, WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR HAVE AT LEAST ONE CFTR MUTATION THAT IS RESPONSIVE TO TEZACAFTOR/IVACAFTOR, WITH AN EFFECTIVE AMOUNT OF TEZACAFTOR AND IVACAFTOR

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	Feb. 12, 2023	NEW CHEMICAL ENTITY
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	Feb. 12, 2025	TREATMENT OF PATIENTS WITH CYSTIC FIBROSIS AGED 12 YEARS AND OLDER WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR WHO HAVE AT LEAST ONE MUTATION IN THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR GENE RESPONSIVE TO TEZACAFTOR/IVACAFTOR
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	June 21, 2026	TX OF PTS W/ CYSTIC FIBROSIS (CF) AGE 6 TO <12 YRS WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR W/ AT LEAST 1 MUTATION IN CF TRANSMEMBRANE CONDUCTANCE REGULATORY GENE RESPONSIVE TO TEZACAFTOR/IVACAFTOR BASED ON IN VITRO DATA AND/OR CLINICAL EVIDENCE
150MG;150MG, 100MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	Feb. 12, 2018	RX	TABLET	ORAL	Dec. 21, 2027	FOR TREATMENT OF CYSTIC FIBROSIS (CF) IN PATIENTS AGE 6 YEARS AND OLDER WHO HAVE AT LEAST ONE OF THE ADDITIONAL MUTATIONS IN THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR (CFTR) GENE THAT HAVE BEEN IDENTIFIED AS RESPONSIVE TO TEZACAFTOR/IVACAFTOR BASED ON IN VITRO DATA AND IDENTIFIED IN THE APPROVAL ON DECEMBER 21, 2020
75MG;75MG, 50MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	June 21, 2019	RX	TABLET	ORAL	Feb. 12, 2023	NEW CHEMICAL ENTITY
75MG;75MG, 50MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	June 21, 2019	RX	TABLET	ORAL	Feb. 12, 2025	TREATMENT OF PATIENTS WITH CYSTIC FIBROSIS AGED 12 YEARS AND OLDER WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR WHO HAVE AT LEAST ONE MUTATION IN THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR GENE RESPONSIVE TO TEZACAFTOR/IVACAFTOR
75MG;75MG, 50MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	June 21, 2019	RX	TABLET	ORAL	June 21, 2026	TX OF PTS W/ CYSTIC FIBROSIS (CF) AGE 6 TO <12 YRS WHO ARE HOMOZYGOUS FOR THE F508DEL MUTATION OR W/ AT LEAST 1 MUTATION IN CF TRANSMEMBRANE CONDUCTANCE REGULATORY GENE RESPONSIVE TO TEZACAFTOR/IVACAFTOR BASED ON IN VITRO DATA AND/OR CLINICAL EVIDENCE
75MG;75MG, 50MG	SYMDEKO (COPACKAGED)	VERTEX PHARMS INC	N210491	June 21, 2019	RX	TABLET	ORAL	Dec. 21, 2027	FOR TREATMENT OF CYSTIC FIBROSIS (CF) IN PATIENTS AGE 6 YEARS AND OLDER WHO HAVE AT LEAST ONE OF THE ADDITIONAL MUTATIONS IN THE CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR (CFTR) GENE THAT HAVE BEEN IDENTIFIED AS RESPONSIVE TO TEZACAFTOR/IVACAFTOR BASED ON IN VITRO DATA AND IDENTIFIED IN THE APPROVAL ON DECEMBER 21, 2020

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Cystic fibrosis transmembrane conductance regulator	Ion channel	P13569	CFTR_HUMAN	PHARMACOLOGICAL CHAPERONE	EC50	6.57		CHEMBL	DRUG LABEL

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External reference:

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ID	Source
CV6	PDB_CHEM_ID
017465	NDDF
10104	INN_ID
10199	IUPHAR_LIGAND_ID
1999382	RXNORM
33763	MMSL
4037327	VANDF
46199646	PUBCHEM_CID
771596001	SNOMEDCT_US
8RW88Y506K	UNII

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Pharmaceutical products:

None