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DRUG INTERACTIONS WITH TRIKAFTA™ (elexacaftor/tezacaftor/ivacaftor and ivacaftor)

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elexacaftor/tezacaftor/ivacaftor and ivacaftor.

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Drug names in the table that are bold are listed in the full Prescribing Information for SYMDEKO.

Drug names in the table that are bold are listed in the full Prescribing Information for TRIKAFTA.

Drug interaction profiles¹

Clinical considerations for TRIKAFTA are based on drug interaction studies, modeling, other clinical factors, and/or predicted interactions due to elimination pathways. Dose adjustments are required for concomitant use with strong and moderate CYP3A inhibitors.

Drug interaction profiles and dose adjustments
	Dose recommendation		TRIKAFTA interaction
Strong CYP3A inducers including: rifampin, rifabutin, phenobarbital, carbamazepine, phenytoin, St. John’s wort (Hypericum perforatum)	CONCOMITANT USE NOT RECOMMENDED		Reduced exposure of TRIKAFTA expected with strong CYP3A inducers The concomitant use of CYP3A inducers may reduce TRIKAFTA efficacy
Strong CYP3A inhibitors including: ketoconazole, itraconazole, posaconazole, voriconazole, telithromycin, clarithromycin	IN THE MORNING (TWICE A WEEK) DAY 1 elexacaftor 100 mg/ tezacaftor 50 mg/ ivacaftor 75 mg 2 tablets DAY 4^a elexacaftor 100 mg/ tezacaftor 50 mg/ ivacaftor 75 mg 2 tablets NO TABLET IN THE EVENING		Increased exposure of TRIKAFTA expected with strong or moderate CYP3A inhibitors
Moderate CYP3A inhibitors including: fluconazole, erythromycin	ALTERNATE TABLETS EVERY MORNING
	DAY 1 elexacaftor 100 mg/ tezacaftor 50 mg/ ivacaftor 75 mg 2 tablets	DAY 2^b ivacaftor 150 mg 1 tablet
	NO TABLET IN THE EVENING
CYP2C9 substrates including: warfarin, glimepiride, glipizide	Caution and appropriate monitoring should be used with CYP2C9, P-gp, and OATP1B1 and OATP1B3 substrates		Increased exposure of substrates may occur with TRIKAFTA Ivacaftor may inhibit CYP2C9 Ivacaftor or tezacaftor/ivacaftor increases digoxin exposure of other sensitive P-gp substrates Elexacaftor and M23-ELX inhibit OATP1B1 and OATP1B3 in vitro
P-glycoprotein (P-gp) substrates including: digoxin, cyclosporine, everolimus, sirolimus, tacrolimus
OATP1B1 and OATP1B3 substrates including^1,2: statins (atorvastatin, cerivastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin) glyburide, nateglinide, repaglinide

^aContinue dosing with 2 elexacaftor/tezacaftor/ivacaftor tablets twice a week, approximately 3 to 4 days apart.¹
^bContinue dosing with 2 elexacaftor/tezacaftor/ivacaftor tablets and 1 ivacaftor tablet on alternate days.¹
Tablets are not actual size.

Drug interaction profiles and dose adjustments
Strong CYP3A inducers including: Rifampin, Rifabutin, Phenobarbital, Carbamazepine, Phenytoin, St. John’s wort, (Hypericum perforatum)
Dose recomendation	TRIKAFTA interaction
CONCOMITANT USE NOT RECOMMENDED	Reduced exposure of TRIKAFTA expected with strong CYP3A inducers The concomitant use of CYP3A inducers may reduce TRIKAFTA efficacy

Strong CYP3A inhibitors including: ketoconazole, itraconazole, posaconazole, voriconazole, telithromycin, clarithromycin
Dose recomendation	TRIKAFTA interaction
IN THE MORNING (TWICE A WEEK) Day 1 elexacaftor 100 mg/ tezacaftor 50 mg/ ivacaftor 75 mg 2 tablets NO TABLET IN THE EVENING Day 4 elexacaftor 100 mg/ tezacaftor 50 mg/ ivacaftor 75 mg 2 tablets NO TABLET IN THE EVENING	Increased exposure of TRIKAFTA expected with strong or moderate CYP3A inhibitors

Tablets are not actual size.

Moderate CYP3A inhibitors including: fluconazole, erythromycin
Dose recomendation	TRIKAFTA interaction
ALTERNATE TABLETS EVERY MORNING Day 1 elexacaftor 100 mg/ tezacaftor 50 mg/ ivacaftor 75 mg 2 tablets NO TABLET IN THE EVENING Day 2 ivacaftor 150 mg 1 tablet NO TABLET IN THE EVENING	Increased exposure of TRIKAFTA expected with strong or moderate CYP3A inhibitors

Tablets are not actual size.

CYP2C9 substrates warfarin, glimepiride, glipizide

P-glycoprotein (P-gp) substrates digoxin, cyclosporine, everolimus, sirolimus, tacrolimus

OATP1B1 and OATP1B3 substrates statins (atorvastatin, cerivastatin, pitavastatin, pravastatin, rosuvastatin, simvastatin) glyburide, nateglinide, repaglinide

Dose recomendation

TRIKAFTA interaction

Caution and appropriate monitoring should be used with CYP2C9, P-gp, and OATP1B1 and OATP1B3 substrates

Increased exposure of substrates may occur with TRIKAFTA

Ivacaftor may inhibit CYP2C9
Ivacaftor or tezacaftor/ivacaftor increases digoxin exposure and may increase exposure of other sensitive P-gp substrates
Elexacaftor and M23-ELX inhibit OATP1B1 and OATP1B3. Tezacaftor/ivacaftor increases pitavastatin exposure

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View the clinical trials of TRIKAFTA >

Indications and Usage

TRIKAFTA is indicated for the treatment of CF in patients aged 12 years and older who have at least one F508del mutation in the cystic fibrosis transmembrane conductance regulator (CFTR) gene.

If the patient’s genotype is unknown, an FDA-cleared CF mutation test should be used to confirm the presence of at least one F508del mutation.

Important Safety Information

Liver Function Test Elevations

Elevated transaminases have been observed in patients with CF treated with TRIKAFTA. Bilirubin elevations have also been observed with TRIKAFTA treatment. Assessments of liver function tests (ALT, AST, and bilirubin) are recommended prior to initiating TRIKAFTA, every 3 months during the first year of treatment, and annually thereafter. For patients with a history of hepatobiliary disease or liver function test elevations, more frequent monitoring should be considered

In the event of significant elevations in liver function tests e.g. ALT or AST >5x the upper limit of normal (ULN) or ALT or AST >3x ULN with bilirubin >2x ULN, dosing should be interrupted and laboratory tests closely followed until the abnormalities resolve. Following the resolution of liver function test elevations, consider the benefits and risks of resuming treatment

Concomitant Use With CYP3A Inducers

Exposure to ivacaftor is significantly decreased and exposure to elexacaftor and tezacaftor are expected to decrease by the concomitant use of strong CYP3A inducers, which may reduce the therapeutic effectiveness of TRIKAFTA. Co‑administration with strong CYP3A inducers is not recommended

Concomitant Use With CYP3A Inhibitors

Exposure to elexacaftor, tezacaftor, and ivacaftor are increased when co-administered with strong or moderate CYP3A inhibitors. The dose of TRIKAFTA should be reduced when used concomitantly with moderate or strong CYP3A inhibitors

Cataracts

Cases of non-congenital lens opacities have been reported in pediatric patients treated with ivacaftor-containing regimens. Baseline and follow up ophthalmological examinations are recommended in pediatric patients initiating treatment with TRIKAFTA

Pediatric Use

The safety and effectiveness efficacy of TRIKAFTA in patients with CF younger than 12 years of age have not been established

Serious Adverse Reactions

Serious adverse reactions that occurred more frequently in patients treated with TRIKAFTA compared to placebo were rash (1% vs <1%) and influenza (1% vs 0). There were no deaths in Trials 1 and 2

Most Common Adverse Reactions

The most common adverse reactions occurring in ≥8% of patients treated with TRIKAFTA (N=202) and at a frequency higher than for placebo (N=201) by ≥1% in the 24 week placebo-controlled, parallel-group Phase 3 trial (Trial 1) were headache, diarrhea, upper respiratory tract infection, abdominal pain, alanine aminotransferase increased, nasal congestion, blood creatine phosphokinase increased, aspartate aminotransferase increased, rash, and rhinorrhea
The safety profile for the patients receiving TRIKAFTA (N=55) in the 4-week, randomized, double-blind, active-controlled Phase 3 trial (Trial 2) was similar to that observed in Trial 1

Click here to access full Prescribing Information for TRIKAFTA.

Indications and Usage

TRIKAFTA is indicated for the treatment of CF in patients aged 12 years and older who have at least one F508del mutation in the cystic fibrosis transmembrane conductance regulator (CFTR) gene.

If the patient’s genotype is unknown, an FDA-cleared CF mutation test should be used to confirm the presence of at least one F508del mutation.

Important Safety Information

Liver Function Test Elevations

In the event of significant elevations in liver function tests e.g. ALT or AST >5x the upper limit of normal (ULN) or ALT or AST >3x ULN with bilirubin >2x ULN, dosing should be interrupted and laboratory tests closely followed until the abnormalities resolve. Following the resolution of liver function test elevations, consider the benefits and risks of resuming treatment

Concomitant Use With CYP3A Inducers

Exposure to ivacaftor is significantly decreased and exposure to elexacaftor and tezacaftor are expected to decrease by the concomitant use of strong CYP3A inducers, which may reduce the therapeutic effectiveness of TRIKAFTA. Co‑administration with strong CYP3A inducers is not recommended

Concomitant Use With CYP3A Inhibitors

Exposure to elexacaftor, tezacaftor, and ivacaftor are increased when co-administered with strong or moderate CYP3A inhibitors. The dose of TRIKAFTA should be reduced when used concomitantly with moderate or strong CYP3A inhibitors

Cataracts

Cases of non-congenital lens opacities have been reported in pediatric patients treated with ivacaftor-containing regimens. Baseline and follow up ophthalmological examinations are recommended in pediatric patients initiating treatment with TRIKAFTA

Pediatric Use

The safety and effectiveness efficacy of TRIKAFTA in patients with CF younger than 12 years of age have not been established

Serious Adverse Reactions

Serious adverse reactions that occurred more frequently in patients treated with TRIKAFTA compared to placebo were rash (1% vs <1%) and influenza (1% vs 0). There were no deaths in Trials 1 and 2

Most Common Adverse Reactions

The most common adverse reactions occurring in ≥8% of patients treated with TRIKAFTA (N=202) and at a frequency higher than for placebo (N=201) by ≥1% in the 24 week placebo-controlled, parallel-group Phase 3 trial (Trial 1) were headache, diarrhea, upper respiratory tract infection, abdominal pain, alanine aminotransferase increased, nasal congestion, blood creatine phosphokinase increased, aspartate aminotransferase increased, rash, and rhinorrhea
The safety profile for the patients receiving TRIKAFTA (N=55) in the 4-week, randomized, double-blind, active-controlled Phase 3 trial (Trial 2) was similar to that observed in Trial 1

Click here to access full Prescribing Information for TRIKAFTA.

DRUG INTERACTIONS WITH TRIKAFTA™ (elexacaftor/tezacaftor/ivacaftor and ivacaftor)

Drug-drug interactions tool1,2

Choose or begin typing the brand or generic drug name or drug class to learn more about potential DDIs

Drug interaction profiles1

Indications and Usage

Important Safety Information

Liver Function Test Elevations

Liver Function Test Elevations

Indications and Usage

Important Safety Information

Liver Function Test Elevations

Liver Function Test Elevations

Drug-drug interactions tool^1,2

Drug interaction profiles¹