IVACAFTOR

Details

Stereochemistry	ACHIRAL
Molecular Formula	C24H28N2O3
Molecular Weight	392.4907
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)(C)C1=CC(=C(NC(=O)C2=CNC3=CC=CC=C3C2=O)C=C1O)C(C)(C)C

InChI

InChIKey=PURKAOJPTOLRMP-UHFFFAOYSA-N

InChI=1S/C24H28N2O3/c1-23(2,3)16-11-17(24(4,5)6)20(27)12-19(16)26-22(29)15-13-25-18-10-8-7-9-14(18)21(15)28/h7-13,27H,1-6H3,(H,25,28)(H,26,29)

HIDE SMILES / InChI

Molecular Formula	C24H28N2O3
Molecular Weight	392.4907
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/203188s017lbl.pdf

Ivacaftor (trade names KALYDECO® (ivacaftor) and ORKAMBI® (lumacaftor/ivacaftor)) is a cystic fibrosis transmembrane conductance regulator potentiator indicated for the treatment of cystic fibrosis in patients age 6 years and older who have one of the following mutations in the CFTR gene: G551D, G1244E, G1349D, G178R, G551S, S1251N, S1255P, S549N, or S549R. One such defect G551D is characterized by a dysfunctional CFTR protein on the cell surface. Although the defective protein is trafficked to the correct area, the epithelial cell surface, while there it cannot transport chloride through the channel. Ivacaftor, a CFTR potentiator, improves the transport of chloride through the ion channel by binding to the channels directly to induce a non-conventional mode of gating which in turn increases the probability that the channel is open. Ivacaftor regulates fluid flow within cells and affects the components of sweat, digestive fluids, and mucus.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Cystic fibrosis transmembrane conductance regulator 6 Target ID: CHEMBL4051 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/203188s017lbl.pdf	Activator 1430		100.0 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Cystic fibrosis 120 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/203188s017lbl.pdf	Primary		Approved 8429	KALYDECO Approved Use KALYDECO is indicated for the treatment of CF in patients age 6 years and older who have an R117H mutation in the CFTR gene Launch Date 2012

C_max

Value	Dose	Co-administered	Analyte	Population
2212 ng/mL EXPERIMENT http://www.concertpharma.com/wp-content/uploads/2015/10/CTP656-Ph1SAD-NACFC-08OCT2015.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:		IVACAFTOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

AUC

Value	Dose	Co-administered	Analyte	Population
44916 ng × h/mL EXPERIMENT http://www.concertpharma.com/wp-content/uploads/2015/10/CTP656-Ph1SAD-NACFC-08OCT2015.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:		IVACAFTOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

T_1/2

Value	Dose	Co-administered	Analyte	Population
15 h EXPERIMENT http://www.concertpharma.com/wp-content/uploads/2015/10/CTP656-Ph1SAD-NACFC-08OCT2015.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:		IVACAFTOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT

Doses

Dose	Population	Adverse events
50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2 years n = 1 Health Status: unhealthy Age Group: 2 years Sex: M Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	Disc. AE: ALT increased... AEs leading to discontinuation/dose reduction: ALT increased (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	Disc. AE: Elevated liver enzymes, Croup... AEs leading to discontinuation/dose reduction: Elevated liver enzymes (2 patients) Croup (1 patient) Sepsis (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
75 mg 2 times / day steady, oral Recommended Dose: 75 mg, 2 times / day Route: oral Route: steady Dose: 75 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	Disc. AE: Elevated liver enzymes, Vomiting... AEs leading to discontinuation/dose reduction: Elevated liver enzymes (1 patient) Vomiting (2 patients) Gastroenteritis (1 patient) Retching (1 patient) Rash (1 patient) Cough increased (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
450 mg 2 times / day multiple, oral Overdose Dose: 450 mg, 2 times / day Route: oral Route: multiple Dose: 450 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207925s000lbl.pdf	healthy, adult Health Status: healthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207925s000lbl.pdf	Other AEs: Dizziness, Diarrhea... Other AEs: Dizziness Diarrhea Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207925s000lbl.pdf

AEs

AE	Significance	Dose	Population
ALT increased	1 patient Disc. AE	50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2 years n = 1 Health Status: unhealthy Age Group: 2 years Sex: M Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Croup	1 patient Disc. AE	50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Sepsis	1 patient Disc. AE	50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Elevated liver enzymes	2 patients Disc. AE	50 mg 2 times / day steady, oral Recommended Dose: 50 mg, 2 times / day Route: oral Route: steady Dose: 50 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Cough increased	1 patient Disc. AE	75 mg 2 times / day steady, oral Recommended Dose: 75 mg, 2 times / day Route: oral Route: steady Dose: 75 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Elevated liver enzymes	1 patient Disc. AE	75 mg 2 times / day steady, oral Recommended Dose: 75 mg, 2 times / day Route: oral Route: steady Dose: 75 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Gastroenteritis	1 patient Disc. AE	75 mg 2 times / day steady, oral Recommended Dose: 75 mg, 2 times / day Route: oral Route: steady Dose: 75 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Rash	1 patient Disc. AE	75 mg 2 times / day steady, oral Recommended Dose: 75 mg, 2 times / day Route: oral Route: steady Dose: 75 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Retching	1 patient Disc. AE	75 mg 2 times / day steady, oral Recommended Dose: 75 mg, 2 times / day Route: oral Route: steady Dose: 75 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Vomiting	2 patients Disc. AE	75 mg 2 times / day steady, oral Recommended Dose: 75 mg, 2 times / day Route: oral Route: steady Dose: 75 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27	unhealthy, 2-6 years n = 34 Health Status: unhealthy Age Group: 2-6 years Population Size: 34 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2015/207925Orig1s000MedR.pdf Page: p. 27
Diarrhea		450 mg 2 times / day multiple, oral Overdose Dose: 450 mg, 2 times / day Route: oral Route: multiple Dose: 450 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207925s000lbl.pdf	healthy, adult Health Status: healthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207925s000lbl.pdf
Dizziness		450 mg 2 times / day multiple, oral Overdose Dose: 450 mg, 2 times / day Route: oral Route: multiple Dose: 450 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207925s000lbl.pdf	healthy, adult Health Status: healthy Age Group: adult Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/207925s000lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
	inhibitor 1767 inducer 389	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A 214 P-gp 1461 CYP2C8 911 Cav1.2 45 Kv1.5 26 CYP1A2 1524 CYP2A6 707 CYP2B6 810 CYP2C19 1478 CYP2E1 882	CYP3A 191 CYP2C 11 P-gp 1537	CYP1A2 701 CYP2A6 79 CYP2B6 547 CYP2C8 168 CYP2C19 293 CYP3A4/5 124

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 35.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 52.0	no
CYP2A6 739	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 35.0	no
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 52.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 35.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 52.0	no
CYP2C19 1553	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 35.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 52.0	no
CYP2C8 965	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 35.0	no
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 35.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 52.0	no
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 52.0	no
CYP3A4/5 335	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 35.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 6.0	weak [IC50 11 uM]
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 6.0	weak [IC50 3.8 uM]
CYP3A 298	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 3.0	weak [IC50 41 uM]	weak (co-administration study) Comment: ivacaftor increased midazolam exposure 1.5x, cmax 1.38x, auc 1.54x Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 3.0
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 3.0	yes [IC50 0.17 uM]
Kv1.5 41	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 34.0	yes [IC50 3.4 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A 191	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 3.0	major	yes (co-administration study) Comment: ketoconazole increased ivacaftor exposure by 8.5x; fluconazole increased ivacaftor exposure by 3x; rifampin decreased ivacaftor exposure by 9x Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 3.0
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 35.0	no
CYP2C 11	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 6.0	no	no (co-administration study) Comment: rosiglitazone had no effect on cmax and auc of ivacaftor Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 6.0
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 6.0	no	no (co-administration study) Comment: desipramine had no effect on cmax and auc of ivacaftor Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/203188lbl.pdf Page: 6.0

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Cav1.2 49	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 34.0
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2012/203188Orig1s000PharmR.pdf Page: 59.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:66901	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:66901
ChemicalBook	CB32506174	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB32506174
MolPort	MolPort-009-194-229	https://www.molport.com/shop/molecule-link/MolPort-009-194-229
Selleck Chemicals	VX-770	http://www.selleckchem.com/products/VX-770.html
ZINC	ZINC000052509463	http://zinc15.docking.org/substances/ZINC000052509463
eMolecules	32278030	https://www.emolecules.com/cgi-bin/more?vid=32278030

PubMed

Title	Date	PubMed
Rescue of CF airway epithelial cell function in vitro by a CFTR potentiator, VX-770.	2009 Nov 3	19846789
Targeting the basic defect in cystic fibrosis.	2010 Nov 18	21083391
Effect of VX-770 in persons with cystic fibrosis and the G551D-CFTR mutation.	2010 Nov 18	21083385
Probing conformational rescue induced by a chemical corrector of F508del-cystic fibrosis transmembrane conductance regulator (CFTR) mutant.	2011 Jul 15	21602569
Cystic fibrosis transmembrane regulator potentiators as promising cystic fibrosis therapies.	2011 Mar	21303308
A CFTR potentiator in patients with cystic fibrosis and the G551D mutation.	2011 Nov 3	22047557
Cystic fibrosis transmembrane conductance regulator (CFTR) potentiator VX-770 (ivacaftor) opens the defective channel gate of mutant CFTR in a phosphorylation-dependent but ATP-independent manner.	2012 Oct 26	22942289

Patents

Sample Use Guides

In Vivo Use Guide

Adults and pediatric patients age 6 years and older: one 150 mg tablet taken orally every 12 hours with fat-containing food. Reduce dose in patients with moderate and severe hepatic impairment. Reduce dose when co-administered with drugs that are moderate or strong CYP3A inhibitors.

Route of Administration: Oral

In Vitro Use Guide

10 uM ivacaftor increased the channel open probability of all CFTR gating mutations tested, reaching levels equivalent to 30% to 118% of normal CFTR.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:23:47 GMT 2023` Edited by `admin` on `Fri Dec 15 16:23:47 GMT 2023`
Record UNII	1Y740ILL1Z
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

IVACAFTOR

Official Name

English

N-[2,4-Bis(1,1-dimethylethyl)-5-hydroxyphenyl]-4-oxo-1,4-dihydroquinoline-3-carboxamide

Systematic Name

English

ivacaftor [INN]

Common Name

English

ORKAMBI COMPONENT IVACAFTOR

Brand Name

English

TRIKAFTA COMPONENT IVACAFTOR

Brand Name

English

IVACAFTOR COMPONENT OF ORKAMBI

Brand Name

English

IVACAFTOR [VANDF]

Common Name

English

IVACAFTOR [ORANGE BOOK]

Common Name

English

IVACAFTOR [MI]

Common Name

English

3-QUINOLINECARBOXAMIDE, N-(2,4-BIS(1,1-DIMETHYLETHYL)-5-HYDROXYPHENYL)-1,4-DIHYDRO-4-OXO-

Systematic Name

English

IVACAFTOR [USAN]

Common Name

English

VX-770

Code

English

KALYDECO

Brand Name

English

SYMKEVI COMPONENT IVACAFTOR

Brand Name

English

IVACAFTOR COMPONENT OF TRIKAFTA

Brand Name

English

Ivacaftor [WHO-DD]

Common Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

647618

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

WHO-VATC

QR07AX02

Created by admin on Fri Dec 15 16:23:48 GMT 2023 , Edited by admin on Fri Dec 15 16:23:48 GMT 2023

FDA ORPHAN DRUG

228306

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

LIVERTOX

NBK547889

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

EMA ASSESSMENT REPORTS

ORKAMBI (AUTHORIZED: CYSTIC FIBROSIS)

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

EU-Orphan Drug

EU/3/18/2116

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

EMA ASSESSMENT REPORTS

KALYDECO (AUTHORIZED: CYSTIC FIBROSIS)

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

FDA ORPHAN DRUG

577517

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

FDA ORPHAN DRUG

434814

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

NDF-RT

N0000184146

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

WHO-ATC

R07AX30

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

FDA ORPHAN DRUG

638618

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

WHO-ATC

R07AX02

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

WHO-ATC

R07AX31

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

Code System Code Type Description

EVMPD

SUB33103

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

PRIMARY

IUPHAR

4342

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

PRIMARY

LACTMED

Lumacaftor and Ivacaftor

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

PRIMARY

NDF-RT

N0000184145

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

PRIMARY

Chloride Channel Activation Potentiators [MoA]

INN

9263

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

PRIMARY

CHEBI

66901

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

PRIMARY

DRUG CENTRAL

4228

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

PRIMARY

RXCUI

1243041

Created by admin on Fri Dec 15 16:23:48 GMT 2023 , Edited by admin on Fri Dec 15 16:23:48 GMT 2023

PRIMARY

RxNorm

FDA UNII

1Y740ILL1Z

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

PRIMARY

PUBCHEM

16220172

Created by admin on Fri Dec 15 16:23:48 GMT 2023 , Edited by admin on Fri Dec 15 16:23:48 GMT 2023

PRIMARY

USAN

WW-53

Created by admin on Fri Dec 15 16:23:48 GMT 2023 , Edited by admin on Fri Dec 15 16:23:48 GMT 2023

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NDF-RT

N0000185504

Created by admin on Fri Dec 15 16:23:48 GMT 2023 , Edited by admin on Fri Dec 15 16:23:48 GMT 2023

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Cytochrome P450 2C9 Inhibitors [MoA]

NDF-RT

N0000190114

Created by admin on Fri Dec 15 16:23:48 GMT 2023 , Edited by admin on Fri Dec 15 16:23:48 GMT 2023

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Cytochrome P450 3A Inhibitors [MoA]

ChEMBL

CHEMBL2010601

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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SMS_ID

100000126135

Created by admin on Fri Dec 15 16:23:48 GMT 2023 , Edited by admin on Fri Dec 15 16:23:48 GMT 2023

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LACTMED

Elexacaftor, Tezacaftor and Ivacaftor

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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DRUG BANK

DB08820

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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CAS

873054-44-5

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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NDF-RT

N0000185503

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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P-Glycoprotein Inhibitors [MoA]

NCI_THESAURUS

C166523

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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LACTMED

Tezacaftor and Ivacaftor

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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EPA CompTox

DTXSID00236281

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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DAILYMED

1Y740ILL1Z

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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WIKIPEDIA

IVACAFTOR

Created by admin on Fri Dec 15 16:23:48 GMT 2023 , Edited by admin on Fri Dec 15 16:23:48 GMT 2023

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NDF-RT

N0000182141

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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Cytochrome P450 3A4 Inhibitors [MoA]

MERCK INDEX

m6565

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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Merck Index

LACTMED

Ivacaftor

Created by admin on Fri Dec 15 16:23:47 GMT 2023 , Edited by admin on Fri Dec 15 16:23:47 GMT 2023

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Related Record Type Details


					PUO0521HZV

CYTOCHROME P450 3A4

METABOLIC ENZYME -> SUBSTRATE

Comments:

In vitro and clinical studies indicate that ivacaftor is primarily metabolized by CYP3A.

Interaction Type:

MAJOR

Amount:


					805SU96HKF

CYTOCHROME P450 3A5

METABOLIC ENZYME -> SUBSTRATE

Amount:


					6D53G0FD0Z

PLASMA PROTEIN FRACTION (HUMAN)

BINDER->LIGAND

Comments:

Ivacaftor is approximately 99% bound to plasma proteins, primarily to albumin, and also to alpha 1-acid glycoprotein and human gamma-globulin.

Interaction Type:

BINDING

Amount:


					SHA6U5FJZL

DEUTIVACAFTOR

LABELED -> NON-LABELED

Amount:


					1Y740ILL1Z

IVACAFTOR

EXCRETED UNCHANGED

Comments:

There was negligible urinary excretion of ivacaftor as unchanged drug.

Amount:


					PW7453NX3R

CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR

TARGET -> ACTIVATOR

Amount:

Related Record Type Details


					38WUF8D79H

IVACAFTOR CARBOXYLATE

METABOLITE INACTIVE -> PARENT

Interaction Type:

MAJOR

Amount:


					38WUF8D79H

IVACAFTOR CARBOXYLATE

METABOLITE INACTIVE -> PARENT

Amount:


					38WUF8D79H

IVACAFTOR CARBOXYLATE

METABOLITE INACTIVE -> PARENT

Interaction Type:

MAJOR

Amount:


					6F3NVS9Y38

HYDROXYMETHYL-IVACAFTOR

METABOLITE ACTIVE -> PARENT

Interaction Type:

MAJOR

Amount:

Related Record Type Details


					1Y740ILL1Z

IVACAFTOR

ACTIVE MOIETY

Amount:

Name	Property Type	Parameters
Biological Half-life	PHARMACOKINETIC

Volume of Distribution	PHARMACOKINETIC

Tmax	PHARMACOKINETIC	ORAL ADMINISTRATION

Details

SMILES

InChI

DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/203188s017lbl.pdf

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Cmax

AUC

T1/2

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/203188s017lbl.pdf

C_max

T_1/2

Drug as perpetrator