Consumer medicine information

1. Why am I using TAGRISSO?

TAGRISSO contains the active ingredient osimertinib mesilate. TAGRISSO is used to treat adults with a type of cancer called 'non-small cell lung cancer' when the tumour has a defect (mutation) in a gene called EGFR (epidermal growth factor receptor).
For more information, see Section 1. Why am I using TAGRISSO? in the full CMI.

2. What should I know before I use TAGRISSO?

Do not use if you have ever had an allergic reaction to osimertinib mesilate, or any other similar medicines for example other tyrosine kinase inhibitors, or any of the ingredients listed at the end of this leaflet.
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 TAGRISSO? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with TAGRISSO and affect how it works.
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 TAGRISSO?

• The usual dose is one 80 mg tablet per day. Your doctor may however prescribe a different dose such as one 40 mg tablet.

• Continue taking TAGRISSO for as long as your doctor tells you.

5. What should I know while using TAGRISSO?

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. These include diarrhoea, dry skin, skin greying or darkening, rash, pain and redness around the fingernails or hair thinning. However, some serious side effects may need medical attention. These include sudden difficulty in breathing with a cough or fever, sore or red eyes, light sensitivity, blurred vision, rapid or irregular heartbeats, chest discomfort, shortness of breath, fainting, persistent fever, bruising easily, increased tiredness, severe blistering or peeling of skin or skin reactions that look like rings.
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.

1 Name of Medicine

Osimertinib mesilate.

2 Qualitative and Quantitative Composition

Each film-coated tablet contains either 40 mg or 80 mg of osimertinib as the mesilate salt.
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

The 40 mg tablets are round, biconvex, beige, film-coated tablets with a diameter of approximately 9 mm. The tablets are debossed with 'AZ' over '40' on one side and plain on the reverse.
The 80 mg tablets are oval, biconvex, beige, film-coated tablets measuring approximately 7.25 x 14.5 mm. The tablets are debossed with 'AZ 80' on one side and plain on the reverse.

4 Clinical Particulars

4.9 Overdose

In Tagrisso clinical trials a limited number of patients were treated with daily doses of up to 240 mg without dose limiting toxicities. In these studies, patients who were treated with Tagrisso daily doses of 160 mg and 240 mg experienced an increase in the frequency and severity of a number of typical EGFR-induced AEs (primarily diarrhoea and skin rash) compared to the 80 mg dose. There is limited experience with accidental overdoses in humans. All cases were isolated incidents of patients taking an additional daily dose of Tagrisso in error, without any resulting clinical consequences.
There is no specific treatment in the event of Tagrisso overdose, and symptoms of overdose are not established. In the event of an overdose, physicians should follow general supportive measures and should treat symptomatically.
For information on the management of overdose, contact the Poisons Information Centre on 131126 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Osimertinib showed no activity in in vitro bacterial and mouse lymphoma cell mutation assays and in in vivo rat bone marrow micronucleus assays, suggesting that it is neither a mutagen nor a clastogen.
Carcinogenicity. Osimertinib showed no carcinogenic potential when administered orally to Tg rasH2 transgenic mice for 26 weeks. Systemic exposure (AUC) in mice at the highest dose tested (10 mg/kg/day) was less than that in patients at the maximum recommended clinical dose. An increased incidence of proliferative vascular lesions (angiomatous hyperplasia and haemangioma) in the mesenteric lymph node was observed in the rat 104-week carcinogenicity study at exposures 0.2-times the AUC observed at the recommended clinical dose of 80 mg once daily. This is consistent with a vascular response in rats to long term drug exposure and is not predictive of carcinogenic potential for vascular neoplasms in humans. In addition, there was an increased incidence of malignant lymphomas in hemolymphoreticular tissue in male rats at exposures 0.2-times the AUC observed at the recommended clinical dose. The clinical relevance of this finding is not known.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Osimertinib mesilate is a single crystalline form solid, which is slightly soluble in water (3.1 mg/mL at 37°C) and has pKa values of 9.5 (aliphatic amine) and 4.4 (aniline).
Chemical structure. The chemical name of osimertinib mesilate is: N-(2-{2-dimethylaminoethyl-methylamino}- 4-methoxy-5-{[4-(1-methylindol-3-yl) pyrimidin-2-yl]amino}phenyl)prop-2-enamide mesilate salt.
The chemical structure of osimertinib mesilate is:
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSOSIMER.gif Molecular formula: C₂₈H₃₃N₇O₂.CH₄O₃S.
Molecular weight: 595.71.
CAS number. CAS number: 1421373-66-1.

7 Medicine Schedule (Poisons Standard)

Schedule 4.

Summary Table of Changes

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