Consumer medicine information

1. What is APRETUDE and what is it used for?

APRETUDE contains the active ingredient cabotegravir, which belongs to a group of antiretroviral medicines called integrase inhibitors (INIs). APRETUDE is used to reduce the risk of getting HIV infection in people weighing 35 kg or more. This is called pre-exposure prophylaxis (PrEP). For more information, see Section 1. What is APRETUDE and what is it used for? in the full CMI.

2. What should I know before I am given APRETUDE?

Do not use if you have ever had an allergic reaction to cabotegravir or any of the ingredients listed at the end of the CMI. Do not use unless you have had a recent HIV test to confirm you are HIV negative.
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 am given APRETUDE? in the full CMI.

3. What if I am taking other medicines?

Some medicines may interfere with APRETUDE 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 APRETUDE is given to me?

• APRETUDE will be given by a nurse or doctor through an injection in the muscle of your buttock (intramuscular injection (IM)) as a single injection once every 2 months.

• You should be given APRETUDE for as long as your doctor recommends. Do not stop unless your doctor advises you to.

5. What should I know while being given APRETUDE?

6. Are there any side effects?

The following very common side effects may occur when using APRETUDE: headache, diarrhoea, injection site reactions, fever. Contact your doctor promptly if you develop an allergic reaction or if you have liver problems.
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

Film-coated tablets: Cabotegravir (as cabotegravir sodium).
Prolonged-release suspension for injection: Cabotegravir.

2 Qualitative and Quantitative Composition

Cabotegravir is a white to almost white solid.
Film-coated tablets. Apretude tablet contains 30 mg cabotegravir (as cabotegravir sodium).
Prolonged-release suspension for injection. Apretude injection contains 600 mg cabotegravir (as cabotegravir free acid) in 3 mL vial.
List of excipients with known effect. Apretude tablets contain lactose monohydrate.
Apretude injection: none
For the full list of excipients, see Section 6.1 List of Excipients.

3 Pharmaceutical Form

Film-coated tablets. Apretude tablets are white, oval, film-coated, tablets, debossed with 'SV CTV' on one side.
Prolonged-release suspension for injection. Apretude injection is a white to light pink suspension.

4 Clinical Particulars

4.9 Overdose

Symptoms and signs. There is currently no experience of overdose with Apretude.
Treatment. There is no specific treatment for overdose with Apretude. If overdose occurs, the individual should be treated supportively with appropriate monitoring as necessary. Further management should be as clinically indicated or as recommended by the national poisons centre, where available.
Apretude is known to be highly protein bound in plasma; therefore, dialysis is unlikely to be helpful in removal of drug from the body. Management of overdose with Apretude injection should take into consideration the prolonged exposure to drug following an injection (see Section 4.4 Special Warnings and Precautions for Use).
For information on the management of overdose, contact the Poisons Information Centre on 13 11 26 (Australia).

5 Pharmacological Properties

5.3 Preclinical Safety Data

Genotoxicity. Cabotegravir was not mutagenic or clastogenic using in vitro tests in bacteria and cultured mammalian cells, and an in vivo rodent micronucleus assay.
Carcinogenicity. Cabotegravir was not carcinogenic in long term oral studies in the mouse and rat at doses resulting in up to 7-8 and 26 times, respectively (75 mg/kg/day in male mice and rats and 35 mg/kg/day in female mice), the maximum AUC in patients.

6 Pharmaceutical Particulars

6.7 Physicochemical Properties

Cabotegravir sodium. Chemical name: sodium (3S,11aR)-N-[(2,4-difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido [1,2-d]pyrazine-8-carboxamide.
Molecular formula: C₁₉H₁₆F₂N₃NaO₅.
Molecular weight: 427.33 g/mol.
Chemical structure.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSCABOSO.gif CAS number. 1051375-13-3.
Cabotegravir. Chemical name: (3S,11aR)-N-[(2,4-Difluorophenyl)methyl]-6-hydroxy-3-methyl-5,7-dioxo-2,3,5,7,11,11a-hexahydro[1,3]oxazolo[3,2-a]pyrido[1,2-d]pyrazine-8-carboxamide.
Molecular formula: C₁₉H₁₇F₂N₃O₅.
Molecular weight: 405.35 g/mol.
Chemical structure.
https://stagingapi.mims.com/au/public/v2/images/fullchemgif/CSCABOTE.gif CAS number. 1051375-10-0.
Cabotegravir is a white to almost white solid.

7 Medicine Schedule (Poisons Standard)

Schedule 4 - Prescription Only Medicine.

Summary Table of Changes

https://stagingapi.mims.com/au/public/v2/images/fulltablegif/APRETUST.gif