Convenient dosing with TOLSURA

TOLSURA must be taken with food

TOLSURA can be incorporated into patients' mealtime routines

Relative bioavailability of TOLSURA with and without food

1500140013001200110010009008007006005004003002001000Plasma Itraconazole (ng/mL)Time relative to first drug administration (day)1514131211109876543210Fed: TOLSURA 2 x 65 mg capsulesFasted: TOLSURA 2 x 65 mg capsules

20 healthy adult volunteers were dosed with TOLSURA twice daily under fasted and fed conditions to steady-state levels for 14.5 days.1

TOLSURA must be taken with food

Conventional itraconazole capsules must be taken with a full meal and, in certain cases, a can of a non-diet cola

Bioavailability under fed and fasted conditions2

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Pharmacokinetic parameters of itraconazole following administration of TOLSURA 130 mg (2 x 65 mg capsules) given twice daily for 14.5 days under fed and fasted conditions in healthy subjects

Parameter

:

Cmax_ss
(ng/mL)

Fed

Geometric
Mean


1400 ± 600

Ratio (%)


73.7

90% Confidence
Interval


69.0, 77.3

Fasted

Geometric
Mean


1900 ± 900

Parameter

:

Ctrough,ss
(ng/mL)

Fed

Geometric
Mean


1000 ± 300

Ratio (%)


90

90% Confidence
Interval


86.4, 97.0

Fasted

Geometric
Mean


1100 ± 600

Parameter

:

AUCtau
(hr•ng/mL)

Fed

Geometric
Mean


13400 ± 500

Ratio (%)


78.4

90% Confidence
Interval


74.5, 81.9

Fasted

Geometric
Mean


17100 ± 8000

Treatment with TOLSURA and a PPI, such as omeprazole, can increase the systemic exposure of itraconazole1*

Due to the unique SUBA™ technology, TOLSURA is less soluble in the acidic stomach environment1

The absorption of TOLSURA is not reduced in patients with lower gastric acidity, including those taking gastric acid secretion suppressors (eg, H2-receptor antagonists, PPIs)2

Absorption of conventional itraconazole capsules is decreased in subjects with reduced gastric acidity, such as those taking medications like PPIs. As a result, patients are cautioned against taking PPIs within 2 hours of administration of conventional itraconazole capsules3

*Patients taking TOLSURA and PPIs should be monitored for any adverse events.

Bioavailability of TOLSURA capsules coadministered with omeprazole1

Hours after dosing3002001000Concentration (ng/mL)1009080706050403020100TOLSURA 2 x 65 mg capsules fastedTOLSURA 2 x 65 mg capsules + omeprazole 40 mg fasted

The effects of TOLSURA and concomitant use of omeprazole were studied in healthy subjects who were given TOLSURA once a day with or without omeprazole.

Co-administration of omeprazole with TOLSURA increases the systemic exposure to itraconazole. Monitor for adverse reactions.

TOLSURA dose reduction may be necessary

Bioavailability of TOLSURA with PPIs2

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Pharmacokinetics of itraconazole following single-dose administration of TOLSURA 130 mg (2 x 65 mg capsules) alone or with omeprazole 40 mg once daily administered for 7 days under fasted conditions in healthy volunteers1

Parameter

:

AUC
(h•ng/mL)

Treatment A
Mean ± SD


2846.3 ± 1644.4

Treatment
A+B
Mean ± SD


3477.9 ± 1572.6

Treatment
A+B vs
Treatment
A Ratio %


122.2

(90% CI:

108.7–137.3

)

Parameter

:

Cmax
(ng/mL)

Treatment A
Mean ± SD


212.9 ± 119.1

Treatment
A+B
Mean ± SD


278.8 ± 106.8

Treatment
A+B vs
Treatment
A Ratio %


130.9

(90% CI:

111.4–153.8

)

Parameter

:

Tmax*
(h)

Treatment A
Mean ± SD


3.5 (2.0–5.0)

Treatment
A+B
Mean ± SD


3.25 (1.5–5.0)

Treatment
A+B vs
Treatment
A Ratio %


Treatment A: TOLSURA; Treatment B: omeprazole.

*Tmax is given as median (range).

When TOLSURA was co-administered with omeprazole, the mean AUC was 22% higher and mean Cmax 31% higher

Dosing for TOLSURA for each indication2

Blastomycosis

130 mg once daily (2 x 65 mg capsules)

Doses above 130 mg/day should be given in two divided doses

If there is no obvious improvement, or there is evidence of progressive fungal disease, the dose should be increased in 65-mg increments to a maximum of 260 mg daily (4 x 65 mg capsules).

Histoplasmosis

130 mg once daily (2 x 65 mg capsules)

Doses above 130 mg/day should be given in two divided doses

If there is no obvious improvement, or there is evidence of progressive fungal disease, the dose should be increased in 65-mg increments to a maximum of 260 mg daily (4 x 65 mg capsules).

Aspergillosis

130 mg (2 x 65 mg capsules) once daily

260 mg/day [130 mg (2 x 65 mg capsules) twice daily]

In life-threatening situations, a loading dose should be used2

It is recommended, based on pharmacokinetic data, that a loading dose of 130 mg (2 x 65 mg capsules) 3 times daily (390 mg/day) be given for the first 3 days of treatment. Doses above 130 mg/day should be given in 2 divided doses

130 mg (2 x 65 mg capsules)

3 times daily (390 mg/day)

Given for the first 3 days of treatment

Treatment should be continued for a minimum of three months and until clinical parameters and laboratory tests indicate that the active fungal infection has subsided. An inadequate period of treatment may lead to recurrence of active infection

The bioavailability of TOLSURA 65 mg capsules is approximately double that of conventional 100 mg itraconazole capsules2

Although the active substance, pharmaceutical form, and route of administration are the same, due to the increased drug absorption seen with TOLSURA 65 capsules, it should not be used interchangeably with other formulations of itraconazole2

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