Consumer medicine information

Staquis

Crisaborole

BRAND INFORMATION

Brand name

Staquis

Active ingredient

Crisaborole

Schedule

SUMMARY CMI

Staquis^®

Consumer Medicine Information (CMI) summary

The full CMI on the next page has more details. If you are worried about using this medicine, speak to your doctor or pharmacist.

1. Why am I using Staquis?

Staquis contains the active ingredient crisaborole. Staquis is an ointment used on the skin (topical) to treat mild to moderate eczema (atopic dermatitis) in adults and children 2 years of age and older. This medicine belongs to a group of medicines called phosphodiesterase-4 inhibitors.
For more information, see Section 1. Why am I using Staquis? in the full CMI.

2. What should I know before I use Staquis?

Do not use if you have ever had an allergic reaction to crisaborole or any of the ingredients listed at the end of the CMI under Section 7.
Talk to your doctor if you have any other medical conditions, take any other medicines, or are pregnant or plan to become pregnant or are breastfeeding.
For more information, see Section 2. What should I know before I use Staquis? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with Staquis and affect how it works. Do not use Staquis together with other eczema (atopic dermatitis) medicines.
A list of these medicines is in Section 3. What if I am taking other medicines? in the full CMI.

4. How do I use Staquis?

Staquis is for use on skin (topical use) only.
Apply a thin layer of Staquis to the affected areas twice a day, for example, once in the morning and once in the evening. Follow the instructions provided and use Staquis until your doctor tells you to stop.

More instructions can be found in Section 4. How do I use Staquis? in the full CMI.

5. What should I know while using Staquis?

Things you should do	Tell your doctor if Staquis is not making your condition better or if you are worried about any side effects. Staquis may cause mild stinging when first applied to your skin. It is safe to continue use if you experience mild stinging with the first few applications. These symptoms are usually mild and normally subside after a few days of use. If you are about to be started on any new medicine, remind your doctor and pharmacist that you are using Staquis.
Things you should not do	Do not use Staquis to treat any other complaints unless your doctor tells you to. Do not give your medicine to anyone else, even if they have the same condition as you. Do not use this medicine after the expiry date.
Looking after your medicine	Keep your ointment in the tube until it is time to use it. Keep Staquis in a cool dry place where the temperature stays below 25°C.

For more information, see Section 5. What should I know while using Staquis? in the full CMI.

6. Are there any side effects?

The most common side effect of Staquis is application site pain, such as burning or stinging. Staquis may cause allergic reactions at or near the application site, hives or itching, redness or swelling at the application site. If you have any of these symptoms, stop using Staquis and tell your doctor immediately. You may need urgent medical attention.
For more information, including what to do if you have any side effects, see Section 6. Are there any side effects? in the full CMI.

FULL CMI

Staquis^®

Active ingredient: crisaborole

Consumer Medicine Information (CMI)

This leaflet provides important information about using Staquis. You should also speak to your doctor or pharmacist if you would like further information or if you have any concerns or questions about using Staquis.

Where to find information in this leaflet:

1. Why am I using Staquis?
2. What should I know before I use Staquis?
3. What if I am taking other medicines?
4. How do I use Staquis?
5. What should I know while using Staquis?
6. Are there any side effects?
7. Product details

1. Why am I using Staquis?

Staquis contains the active ingredient crisaborole. Staquis is an ointment used on the skin (topical) to treat mild to moderate eczema (atopic dermatitis) in adults and children 2 years of age and older.

This medicine belongs to a group of medicines called phosphodiesterase-4 inhibitors.

Ask your doctor if you have any questions about why this medicine has been prescribed for you. Your doctor may have prescribed it for another reason.

2. What should I know before I use Staquis?

Warnings

Do not use Staquis:

if you are allergic to crisaborole, or any of the ingredients listed at the end of this leaflet under Section 7. Symptoms of an allergic reaction may include:
- shortness of breath
- wheezing or difficulty breathing
- swelling of the face, lips, tongue or other parts of the body
- rash, itching or hives on the skin.
for a condition for which it was not prescribed.
after the expiry date printed on the pack, or if the packaging is torn or show signs of tampering. If you use Staquis after the expiry date has passed, it may have no effect at all, or worse, have an entirely unexpected effect. If it has expired or is damaged, return it to your pharmacist for disposal.

During treatment, you may be at risk of developing certain side effects. It is important you understand these risks and how to monitor for them. See additional information under Section 6. Are there any side effects?

Pregnancy and breastfeeding

Check with your doctor if you are pregnant or intend to become pregnant.

It is not known if Staquis will harm your unborn baby.

Talk to your doctor if you are breastfeeding or intend to breastfeed.

It is not known whether Staquis passes through breast milk. Therefore, if you are breastfeeding, you should discuss with your doctor whether to stop breastfeeding or stop using Staquis.

Children

Staquis is not currently recommended for use in children under 2 years of age as it has not been tested in children under 2 years.

3. What if I am taking other medicines?

Tell your doctor or pharmacist if you are taking any other medicines, including any medicines, vitamins or supplements that you buy without a prescription from your pharmacy, supermarket or health food shop.

Some medicines may interfere with Staquis and affect how it works.

Do not use Staquis together with other eczema (atopic dermatitis) medicines.

Emollients, used to moisturise and soothe dry skin, may be used on other areas of skin whilst using Staquis. Talk to your doctor about how to use emollients whilst using Staquis.

Check with your doctor or pharmacist if you are not sure about what medicines, vitamins or supplements you are taking and if these affect Staquis.

Your doctor and pharmacist have more information on medicines to be careful with or avoid while using this medicine.

4. How do I use Staquis?

How much to use

Apply a thin layer of Staquis to the affected areas twice a day, for example, once in the morning and once in the evening.
Follow the instructions provided and use Staquis until your doctor tells you to stop.

How long to use it

Continue using this medicine for as long as your doctor tells you. This medicine helps to control your condition, but does not cure it.

How to use it

Staquis is for use on skin (topical use) only.
Do not use Staquis in your eyes, mouth, or vagina.
Staquis, due to its thick formulation, may not be ideal for use on the scalp (with hair).
Squeeze out enough Staquis from the tube to cover the affected areas with a layer of the ointment.
Rub the ointment into skin thoroughly.
Apply only in one direction on hairy skin to avoid causing skin irritation or inflammation.
If someone else applies Staquis for you, they should wash their hands after applying Staquis.
Do not swim, bathe, shower or wash off Staquis for at least 4 hours after dosing. DO NOT reapply any until your next scheduled dosing time.

If you forget to use Staquis

If you miss a dose, apply Staquis when you remember, if it is at least 8 hours before the next scheduled dosing. Otherwise, skip the missed dose and apply the next dose at the normally scheduled time.
Do not use a double dose to make up for the dose that you missed.
If you are unsure what to do, ask your doctor or pharmacist.

If you use too much Staquis

If you accidentally apply more Staquis to your skin than you were told to, wipe off the excess. It will not harm you.

If you or anyone else swallows some of the ointment, you may need urgent medical attention.

You should immediately:

phone the Poisons Information Centre
(by calling 13 11 26), or
contact your doctor, or
go to the Emergency Department at your nearest hospital.

You should do this even if there are no signs of discomfort or poisoning.

5. What should I know while using Staquis?

Things you should do

Follow all directions given to you by your doctor or pharmacist carefully. They may differ from the information contained in this leaflet.
If you do not understand the instructions on the pack, ask your doctor or pharmacist for help.
Tell your doctor if Staquis is not making your condition better or if you are worried about any side effects. Staquis may cause mild stinging when first applied to your skin. It is safe to continue use if you experience mild stinging with the first few applications. These symptoms are usually mild and normally subside after a few days of use.
If you are about to be started on any new medicine, remind your doctor and pharmacist that you are using Staquis.

Things you should not do

Do not use Staquis to treat any other complaints unless your doctor tells you to.
Do not give your medicine to anyone else, even if they have the same condition as you. It may harm them.

Driving or using machines

This medicine is not expected to affect your ability to drive a car or operate machinery.

Looking after your medicine

Keep your ointment in the tube until it is time to use it. If you take the ointment out of the tube, it might not keep well.
Keep Staquis in a cool dry place where the temperature stays below 25°C.

Do not store Staquis or any other medicine:

in the bathroom or near a sink, or
in the car or on window sills.

Heat and dampness can destroy some medicines.

Keep it where young children cannot reach it.

A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.

When to discard your medicine

Do not use this medicine after the expiry date.

If your doctor tells you to stop using this medicine or the expiry date has passed, ask your pharmacist what to do with any medicine that is left over.

Getting rid of any unwanted medicine

If you no longer need to use this medicine or it is out of date, take it to any pharmacy for safe disposal.

6. Are there any side effects?

All medicines can have side effects. If you do experience any side effects, most of them are minor and temporary. However, some side effects may need medical attention.

See the information below and, if you need to, ask your doctor or pharmacist if you have any further questions about side effects.

This medicine helps most people with atopic dermatitis, but it may have unwanted side effects in a few people. All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical attention if you get some of the side effects.

Do not be alarmed by the following list of side effects. You may not experience any of them.

Common side effects

Common side effects	What to do
application site pain, such as burning or stinging	Speak to your doctor if you have any of these common side effects and they worry you.

Serious side effects

Serious side effects	What to do
allergic reaction at or near the application site - signs of an allergic reaction such as swelling of the face, lips or tongue which may cause difficulty in swallowing or breathing hives or itching redness or swelling at the application site	Call your doctor straight away, or go straight to the Emergency Department at your nearest hospital if you notice any of these serious side effects. If you have any of these symptoms, stop using Staquis.

Tell your doctor or pharmacist if you notice anything else that may be making you feel unwell.

Do not be alarmed by this list of side effects. You may not experience any of them. Other side effects not listed here may occur in some people.

Reporting side effects

After you have received medical advice for any side effects you experience, you can report side effects to the Therapeutic Goods Administration online at www.tga.gov.au/safety/reporting-problems. By reporting side effects, you can help provide more information on the safety of this medicine.

Always make sure you speak to your doctor or pharmacist before you decide to stop taking any of your medicines.

7. Product details

This medicine is only available with a doctor's prescription.

This medicine is not addictive.

What Staquis contains

Active ingredient (main ingredient)	crisaborole 2% (w/w)
Other ingredients (inactive ingredients)	white soft paraffin propylene glycol glyceryl monostearate synthetic paraffin butylated hydroxytoluene sodium calcium edetate

Do not take this medicine if you are allergic to any of these ingredients.

This medicine does not contain lactose, sucrose, gluten, tartrazine or any other azo dyes.

What Staquis looks like

Staquis is a white to off-white ointment in a tube.

AUST R 295283.

Staquis is available in a 60g tube.

Who distributes Staquis

Pfizer Australia Pty Ltd
Sydney NSW
Toll Free Number: 1800 675 229
www.pfizermedicalinformation.com.au

This leaflet was prepared in January 2025.

Published by MIMS February 2025

BRAND INFORMATION

Brand name

Staquis

Active ingredient

Crisaborole

Schedule

1 Name of Medicine

Crisaborole.

2 Qualitative and Quantitative Composition

Staquis contains 2% (w/w) crisaborole in a paraffin-based, ointment and is for topical use. The active ingredient, crisaborole, is a phosphodiesterase-4 (PDE-4) inhibitor. Each gram of Staquis contains 20 mg of crisaborole.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Staquis is a white to off-white ointment containing 20 mg of crisaborole per gram (2% w/w) crisaborole.

4 Clinical Particulars

4.1 Therapeutic Indications

Staquis is indicated for topical treatment of mild to moderate atopic dermatitis in patients 2 years of age and older.

4.2 Dose and Method of Administration

Dosage.

Staquis can be used continuously for up to 28 days per treatment course. The efficacy for continuous use beyond 28 days has not been studied in a controlled trial. Multiple treatment courses over 48 weeks have been studied in an open-label extension trial. Do not co-apply Staquis with other topical atopic dermatitis medicines on the same lesions. The concurrent use of Staquis with other topical atopic dermatitis medicines on separate lesions has not been studied.

Adults.

Staquis is to be applied as a thin layer twice daily to affected areas. Staquis can be used on all skin areas, including the head and face, neck and intertriginous areas. Use on the scalp has not been studied.

Paediatric population.

For children and adolescents (2-17 years) the dosage is the same as for adults. The safety and efficacy of Staquis in children less than 2 years of age has not been established. No data are available.

Method of administration.

Staquis is for topical use only and not for oral, ophthalmic, or intravaginal use. If accidentally applied to these areas, the ointment should be thoroughly wiped off and rinsed well with water.
Patients should be instructed to wash their hands after applying Staquis, unless it is their hands that are being treated. If someone else applies Staquis to the patient, they too should wash their hands after application.

4.3 Contraindications

Staquis is contraindicated in patients with known hypersensitivity to crisaborole or any component of the formulation (see Section 4.4).

4.4 Special Warnings and Precautions for Use

Hypersensitivity reactions.

Hypersensitivity reactions, including contact urticaria, have occurred in patients treated with Staquis. Hypersensitivity should be suspected in the event of severe pruritus, swelling and erythema at the application site or at a distant site. If signs and symptoms of hypersensitivity occur, discontinue Staquis immediately and initiate appropriate therapy.

Use in hepatic impairment.

Clinical studies with hepatic impaired subjects have not been conducted.

Use in renal impairment.

Clinical studies with renal impaired subjects have not been conducted.

Use in the elderly.

Clinical studies of Staquis did not include sufficient numbers of subjects aged 65 years and over to determine whether they respond differently from younger subjects.

Paediatric use.

The safety and effectiveness of Staquis have been established in paediatric patients age 2 years and older for topical treatment of mild to moderate atopic dermatitis. Use of Staquis in this age group is supported by evidence from two multicentre, randomised, double-blind, parallel-group, vehicle-controlled 28-day trials which included 1,313 paediatric subjects 2 years and older (see Section 5.1 Pharmacodynamic Properties, Clinical trials; Section 4.8 Adverse Effects (Undesirable Effects)). The safety and effectiveness of Staquis in paediatric patients below the age of 2 years have not been established.

Effects on laboratory tests.

No data available.

Class effects of oral PDE-4 inhibitors.

Insomnia, anxiety, depression, suicidal ideation and weight loss are observed as risks in patients taking oral PDE-4 inhibitors. Existing data from clinical trials and post marketing experience with topical crisaborole do not show evidence of a similar risk with Staquis.

4.5 Interactions with Other Medicines and Other Forms of Interactions

Drug interaction studies.

In vitro studies using human liver microsomes indicated that under the conditions of clinical use, crisaborole and metabolite 1 are not expected to inhibit cytochrome P450 (CYP) 1A2, 2B6, 2C8, 2C9, 2C19, 2D6, and 3A4.
In vitro human liver microsomes studies for metabolite 2 showed that it did not inhibit activities of CYP2C19, 2D6, and 3A4; was a weak inhibitor of CYP1A2 and 2B6; and a moderate inhibitor of CYP2C8 and 2C9. The most sensitive enzyme, CYP2C9, was further investigated in a clinical trial using warfarin as a CYP2C9 substrate. The results of this study showed no drug interaction potential.
In vitro studies in human hepatocytes showed that under the conditions of clinical use, crisaborole and metabolites 1 and 2 are not expected to induce CYP enzymes.
Staquis has not been evaluated in combination with other topical drugs used to treat mild to moderate atopic dermatitis. Emollients may be used on areas of skin other than skin concurrently treated with Staquis.

4.6 Fertility, Pregnancy and Lactation

Effects on fertility.

No effects on fertility were observed in male or female rats that were administered oral doses up to 600 mg/kg/day crisaborole (13 times the maximum recommended human dose (MRHD) on an AUC comparison basis).
(Category B1)
There are no adequate data from the use of crisaborole in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity at maternally non-toxic doses. Because animal reproduction studies are not always predictive of the human response, as a precautionary measure, the mother's clinical benefit of Staquis along with any potential risk on the fetus should be considered.
In animal reproduction studies, rat and rabbit embryo-fetal development was assessed after oral administration of crisaborole. Crisaborole did not cause adverse effects to the fetus at oral doses up to 300 mg/kg/day in pregnant rats during the period of organogenesis (3 times the MRHD on an AUC comparison basis). No drug-related fetal malformations were noted after oral administration of crisaborole in pregnant rats at doses up to 600 mg/kg/day (13 times the MRHD on an AUC comparison basis) during the period of organogenesis. Maternal toxicity was produced at the high dose of 600 mg/kg/day in pregnant rats and was associated with findings of decreased fetal body weight and delayed skeletal ossification. Crisaborole did not cause adverse effects to the fetus at oral doses up to the highest dose tested of 100 mg/kg/day in pregnant rabbits during the period of organogenesis (2 times the MRHD on an AUC comparison basis).
In a prenatal/postnatal development study, pregnant rats were treated with crisaborole at doses of 150, 300, or 600 mg/kg/day by oral gavage during gestation and lactation (from gestation day 7 through day 20 of lactation). Crisaborole did not have any adverse effects on fetal development at doses up to 300 mg/kg/day (3 times the MRHD on an AUC comparison basis). Maternal toxicity was produced at the high dose of 600 mg/kg/day in pregnant rats and was associated with findings of stillbirths, pup mortality, and reduced pup weights.
There is no information available on the presence of crisaborole in human milk, the effects of the drug on the breastfed infant or the effects of the drug on milk production after topical application of Staquis to women who are breastfeeding. Crisaborole is systemically absorbed. The lack of clinical data during lactation precludes a clear determination of the risk of Staquis to a breastfed infant. Therefore, the developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for Staquis and any potential adverse effects on the breastfed infant from Staquis or from the underlying maternal condition. To avoid unintentional ingestion by the newborn, Staquis should not be applied to the breast.

4.7 Effects on Ability to Drive and Use Machines

Staquis has no known influence on the ability to drive and use machines.

4.8 Adverse Effects (Undesirable Effects)

Clinical trials experience.

Two multicentre, randomised, double-blind, parallel-group, vehicle-controlled trials (studies 301 and 302) included a total of 1,522 subjects 2 to 79 years of age (86.3% of subjects were 2 to 17 years of age) and one multicentre, single-arm, open-label long-term safety trial (study 303) included a total of 517 subjects 2 to 72 years of age; in all three trials, subjects treated 5% to 95% body surface area.
The number of subjects with at least 4 weeks, 24 weeks, and 48 weeks of cumulative exposure to Staquis was 1025, 272, and 20, respectively.
In the 28-day pivotal trials, application site pain (e.g. burning or stinging) was the only treatment-related adverse event that showed a clinically relevantly higher rate in Staquis-treated groups versus vehicle-treated groups in subjects with atopic dermatitis. Generally, application site pain was noted early in the treatment period and was transient in nature, resolving spontaneously.
Treatment-emergent adverse events reported by ≥ 1% of subjects from either treatment group, based on the pooled safety population (studies 301 and 302) are listed in Table 1.

Uncommon (< 1%) adverse reactions in subjects treated with Staquis included contact urticaria (see Section 4.4 Special Warnings and Precautions for Use).

Open-label clinical trial experience (exposure up to 48 weeks).

The safety profile from a completed Staquis open-label clinical trial (study 303) in which Staquis was applied intermittently in 28 day treatment courses for up to 48 weeks was consistent with that of studies 301 and 302 (see Section 5.1 Pharmacodynamic Properties, Clinical trials). See Table 2.

Post-market experience.

The safety profile from post-market experience is consistent with that established through clinical trial experience. No new safety information has been derived from the post-market experience.

Reporting suspected adverse effects.

Reporting suspected adverse reactions after registration of the medicinal product is important. It allows continued monitoring of the benefit-risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions at http://www.tga.gov.au/safety/reporting-problems.

4.9 Overdose

There has been no experience of overdose with Staquis. Overdose following topical administration is unlikely. If too much Staquis has been applied, the excess can be wiped off.
Staquis is not for oral use. Oral ingestion may lead to adverse effects associated with systemic administration. If oral ingestion occurs, medical advice should be sought.
For information on the management of overdose, contact the Poison Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.1 Pharmacodynamic Properties

Mechanism of action.

Crisaborole is a competitive inhibitor of cyclic adenosine monophosphate (cAMP) at the PDE-4 catalytic site resulting in increased intracellular cAMP levels. As a phosphodiesterase-4 (PDE-4) inhibitor, crisaborole suppresses inflammation and secretion of certain cytokines, such as TNF α, from the peripheral blood mononuclear cells. The specific mechanism(s) by which crisaborole exerts its therapeutic action for the treatment of atopic dermatitis is not well defined.

Clinical trials.

Two multicentre, randomised, double-blind, parallel-group, vehicle-controlled trials (studies 301 and 302) treated a total of 1,522 subjects 2 to 79 years of age (86.3% of subjects were 2 to 17 years of age) with a 5% to 95% treatable body surface area. At baseline, 38.5% of the subjects had an Investigator's Static Global Assessment [ISGA] score of 2 (mild), and 61.5% had an ISGA score of 3 (moderate), in the overall assessment of atopic dermatitis (erythema, induration/papulation, and oozing/crusting) on a severity scale of 0 to 4.
In both trials, subjects were randomised 2:1 to receive Staquis or vehicle applied twice daily for 28 days. The primary efficacy endpoint was the proportion of subjects at day 29 who achieved success, defined as an ISGA grade of clear (score of 0) or almost clear (score of 1) with a 2-grade or greater improvement from baseline, comparing Staquis-treated subjects to vehicle-treated subjects. The success rates over time are presented in Figure 1.
In both trials, a statistically significantly greater percentage of subjects achieved the success in ISGA in the Staquis-treated group compared with the vehicle-treated group. The proportion of subjects achieving an ISGA score of clear (0) or almost clear (1) at day 29 in the Staquis-treated group compared to the vehicle-treated group was also statistically significant. The secondary efficacy endpoints were the proportion of subjects at day 29 with ISGA grade of clear (score of 0) or almost clear (score of 1) and the time to success in ISGA. Efficacy results from the two trials are summarised in Table 3.

A log-rank test showed the Staquis-treated group had a statistically significantly earlier time to success in ISGA than the vehicle-treated group in both studies (p-values < 0.001).

The incidence of flare and relapse has not been established in controlled trials. Currently, there are no clinical trial data comparing crisaborole to an active comparator.

5.2 Pharmacokinetic Properties

Absorption.

The pharmacokinetics (PK) of Staquis were investigated in 33 paediatric subjects 2 to 17 years of age with mild to moderate atopic dermatitis and a mean ± SD body surface area involvement of 49 ± 20% (range 27% to 92%). In this study, subjects applied approximately 3 mg/cm² of Staquis ointment (dose range was approximately 6 g to 30 g per application) twice daily for 8 days.
Plasma concentrations were quantifiable in all the subjects. When Staquis ointment is applied topically, approximately 25% of the crisaborole dose is absorbed. The mean ± SD maximum plasma concentration (C_max) and area under the concentration time curve from 0 to 12 hours post dose (AUC_0-12) for crisaborole on day 8 were 127 ± 196 nanogram/mL and 949 ± 1240 nanogram*h/mL, respectively. Systemic concentrations of crisaborole were at steady state by day 8. Based on the ratios of AUC_0-12 between day 8 and day 1, the mean accumulation factor for crisaborole was 1.9. Systemic levels of crisaborole and its main metabolites were similar between age cohorts of 2 - 5 years, 6 - 11 years, and 12 - 17 years.

Distribution.

Based on an in vitro study, crisaborole is 97% bound to human plasma proteins.

Metabolism.

After dermal absorption, crisaborole is substantially and rapidly metabolised into inactive metabolites. The major metabolite 5-(4-cyanophenoxy)-2-hydroxyl benzylalcohol (metabolite 1), is formed via hydrolysis; this metabolite is further metabolised into downstream metabolites, among which 5-(4-cyanophenoxy)-2-hydroxyl benzoic acid (metabolite 2), formed via oxidation, is also a major metabolite.
PK of metabolites 1 and 2 were assessed in the PK study described above and the systemic concentrations were at or near steady state by day 8. Based on the ratios of AUC_0-12 between day 8 and day 1, the mean accumulation factors for metabolites 1 and 2 were 1.7 and 6.3, respectively.

Excretion.

Renal excretion of metabolites is the major route of elimination.

5.3 Preclinical Safety Data

Genotoxicity.

Crisaborole revealed no evidence of mutagenic or clastogenic potential based on the results of two in vitro genotoxicity tests (Ames assay and human lymphocyte chromosomal aberration assay) and one in vivo genotoxicity test (rat micronucleus assay).

Carcinogenicity.

In an oral carcinogenicity study in Sprague-Dawley rats, oral doses of 30, 100 or 300 mg/kg/day crisaborole were administered to rats once daily. A drug-related increased incidence of benign granular cell tumours in the uterus with cervix or vagina (combined) was noted in 300 mg/kg/day crisaborole administered female rats (2 times the MRHD on an AUC comparison basis). Given the tumour type and benign nature in a single species and single sex, the relevance to humans is considered to be low.
In a dermal carcinogenicity study in CD-1 mice, topical doses of 2%, 5% and 7% crisaborole ointment were administered once daily. No drug-related neoplastic findings were noted at topical doses up to 7% crisaborole ointment (equal to the MRHD on an AUC comparison basis).

6 Pharmaceutical Particulars

6.1 List of Excipients

Staquis ointment also contains white soft paraffin, propylene glycol, glyceryl monostearate, synthetic paraffin, butylated hydroxytoluene, and sodium calcium edetate.

6.2 Incompatibilities

Incompatibilities were either not assessed or not identified as part of the registration of this medicine.

6.3 Shelf Life

In Australia, information on the shelf life can be found on the public summary of the ARTG. The expiry date can be found on the packaging.

6.4 Special Precautions for Storage

Store below 25°C.

6.5 Nature and Contents of Container

Staquis is supplied in 2.5 g x 6*, 30 g*, 60 g and 100 g* multi-layered laminate tubes with a high density polyethylene tube head with a peel seal, and a white polypropylene cap closure.
* Not all pack sizes available.

6.6 Special Precautions for Disposal

In Australia, any unused medicine or waste material should be disposed of in accordance with local requirements.

6.7 Physicochemical Properties

Crisaborole is described chemically as 5-(4-cyanophenoxy)-1,3-dihydro-1-hydroxy-[2,1]-benzoxaborole. The empirical formula is C₁₄H₁₀BNO₃ and the molecular weight is 251.1 g/mol.
Crisaborole drug substance is freely soluble in common organic solvents such as isopropyl alcohol and propylene glycol, and insoluble in water.

Chemical structure.

The structural formula is represented below:

CAS number.

906673-24-3.

7 Medicine Schedule (Poisons Standard)

Prescription Only Medicine (S4).

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Staquis

Crisaborole

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BRAND INFORMATION