Patient leaflets and SmPCs, drug interaction checker, official dosages and NHS pharmacy opening hours — all in one place.
Patient leaflets and SmPCs, drug interaction checker, official dosages and NHS pharmacy opening hours — all in one place.
The electronic medicines compendium (emc) no longer publishes a Summary of Product Characteristics for this product, which usually means it is no longer marketed in the UK. The patient leaflet below is kept for reference, but the product may not be available.
If you were prescribed this medicine, other products containing Cabotegravir may still be available. Do not stop your treatment — ask your pharmacist or GP what to use instead.
for
Apretude contains the active ingredient cabotegravir. Cabotegravir belongs to a group of antiretroviral medicines called integrase inhibitors (INIs). Apretude is used to help prevent HIV-1 infection in adults and adolescents weighing at least 35kg who are at an increased risk of infection. This is called pre-exposure prophylaxis: PrEP (see section 2). It should be used in combination with safer sex practices, such as use of condoms. 2.
Apretude
Do not use Apretude: if you are allergic (hypersensitive) to cabotegravir or any of the other ingredients of this medicine (listed in section 6). If you are HIV positive or you do not know if you are HIV positive. Apretude can only help reduce your risk of getting HIV before you are infected. You must get tested to make sure you are HIV negative before taking Apretude. if you are taking any of the following medicines:
1
Just taking Apretude may not prevent HIV infection. HIV infection is spread by sexual contact with someone who is HIV positive or by transfer of infected blood. Although Apretude lowers the risk of becoming infected, you can still get HIV when taking this medicine. Other measures should be taken to further reduce your risk of getting HIV:
2
Children and adolescents This medicine should not be used in children or adolescents weighing less than 35 kg, because it has not been studied in these individuals. Other medicines and Apretude Tell your doctor if you are taking, have recently taken or might take any other medicines, including other medicines bought without a prescription. Some medicines can affect how Apretude works or make it more likely that you will have side effects. Apretude can also affect how some other medicines work. Apretude must not be given with some other medicines that may affect how well the medicine works (see 'Do not use Apretude' in section 2). These include:
3
This medicine is given as a 600 mg injection. A nurse or doctor will give you Apretude in the muscle of your buttock. You must have a HIV-negative test before being given Apretude. You will be given your first and second dose of Apretude one month apart. After the second dose, you will be given Apretude as a single injection once every 2 months. Before starting treatment with Apretude injections, you and your doctor may decide first take cabotegravir tablets (called oral lead-in period). The lead-in period allows you and your doctor to assess whether it's appropriate to proceed with injections. If you decide to start treatment with tablets:
Which medicine
First and second injection one month apart Third injection onwards, every two months
Apretude 600 mg Apretude 600 mg
If you are given too much Apretude injection A doctor or nurse will give this medicine to you, so it is unlikely that you will be given too much. If you are worried, tell the doctor or nurse and you will be treated as needed. If you miss a Apretude injection Contact your doctor immediately to make a new appointment. It is important that you keep your regular planned appointments to receive your injection and reduce the risk of getting HIV (see section 2). Talk to your doctor if you are thinking about stopping Apretude. Talk to your doctor if you think you will not be able to receive your Apretude injection at the usual time. Your doctor may recommend you take cabotegravir tablets instead, until you are able to receive an Apretude injection again. Don't stop receiving Apretude injections without advice from your doctor. Keep receiving Apretude injections for as long as your doctor recommends. Don't stop unless your doctor advises you to. If you stop and you are still at risk of getting HIV your doctor must start you on another PrEP medicine within 2 months of your last Apretude injection. If you have any further questions on the use of this medicine, ask your doctor or pharmacist. 4.
Like all medicines, this medicine can cause side effects, although not everybody gets them. 4
Allergic reactions Apretude contains cabotegravir, which is an integrase inhibitor. Integrase inhibitors including cabotegravir can cause a serious allergic reaction known as a hypersensitivity reaction. If you get any of the following symptoms:
5
• •
liver damage (hepatotoxicity). Signs may include yellowing of the skin and the whites of the eyes, loss of appetite, itching, tenderness of the stomach, light-coloured stools or unusually dark urine. Increase in blood bilirubin, a breakdown product of red blood cells, as measured in blood tests.
Very rare side effects (may affect up to 1 in 10,000 people)
Apretude
Keep this medicine out of the sight and reach of children. Do not use this medicine after the expiry date which is stated on the label and carton after EXP. The expiry date refers to the last day of that month. The doctor or nurse is responsible for storing this medicine correctly. Do not freeze. 6.
What Apretude contains The active substance is cabotegravir. Each 3 ml vial contains 600 mg cabotegravir. The other ingredients are: Mannitol (E421) Polysorbate 20 (E432) Macrogol (E1521) Water for injections What Apretude looks like and contents of the pack Cabotegravir is a white to light pink suspension, presented in a brown glass vial with a rubber stopper and an aluminium overseal with a plastic flip-cap. Marketing Authorisation Holder ViiV Healthcare UK Limited 79 New Oxford Street London WC1A 1DG United Kingdom 6
Manufacturer Glaxo Operations UK Limited (trading as Glaxo Wellcome Operations) Harmire Road Barnard Castle County Durham DL12 8DT United Kingdom Other formats To listen to or request a copy of this leaflet in Braille, large print or audio please call, free of charge:
0800 198 5000 (UK Only) Please be ready to give the following information: Product name Reference number
Apretude 600 mg Injection 35728/0062
This is a service provided by the Royal National Institute of Blind People. This leaflet was last revised in April 2025. ————————————————————————————————————————
The following information is intended for healthcare professionals only: Apretude 600 mg prolonged-release suspension for injection cabotegravir For intramuscular use Instructions for Use 3 ml
Overview At each visit, one injection is required; cabotegravir 3 mL (600mg). Cabotegravir is a suspension that does not need further dilution or reconstitution.
7
Cabotegravir is for intramuscular use only. It must be administered to the gluteal sites. Note: The ventrogluteal site is recommended.
Storage information
1 Luer-Lock syringe (5 mL)
•
1 Luer-Lock aspiration needle or aspiration device (to draw up the suspension)
To administer the injection •
1 additional Luer-Lock needle (use safety needle if available) of 23 gauge, 1.5 inches
Consider the patient's build and use medical judgment to select an appropriate injection needle length.
8
You will also need •
Non-sterile gloves
•
2 alcohol swabs
•
1 gauze pad
•
A suitable sharps container
Preparation 1. Inspect vial
MONTH/YEAR
EXP
Check expiry date and medicine
Note: The cabotegravir vial has a brown tint to the glass.
2. Shake vigorously 10 sec
•
Hold the vial firmly and vigorously shake for a full 10 seconds as shown.
•
Invert the vial and check the resuspension. It should look uniform. If the suspension is not uniform, shake the vial again.
•
It is normal to see small air bubbles.
•
Remove the cap from the vial.
•
Wipe the rubber stopper with an alcohol swab.
Do not allow anything to touch the rubber stopper after wiping it. 3. Prepare syringe and needle
9
10
4. Slowly draw up dose
Note: Check that the suspension looks uniform and white to light pink.
5. Attach injection needle
Injection 6. Prepare injection site Injections must be administered to the gluteal sites. Select from the following areas for the injection: • •
Ventrogluteal
Dorsogluteal
11
Ventrogluteal (recommended) Dorsogluteal (upper outer quadrant)
Note: For gluteal intramuscular use only. Do not inject intravenously.
7. Remove extra liquid
8. Stretch skin Use the z-track injection technique to minimise medicine leakage from the injection site.
1 inch (2.5 cm)
9. Inject dose
10. Assess the injection site
12
13
Questions and Answers 1. If the pack has been stored in the refrigerator, is it safe to warm the vial up to room temperature more quickly? You should wait at least 15 minutes before you are ready to give the injection to allow the medicine to reach room temperature. It is best to let the vial come to room temperature naturally. However, you can use the warmth of your hands to speed up the warm-up time, but make sure the vial does not get above 30°C. Do not use any other heating methods. 2. How long can the medicine be left in the syringe? It is best to inject the (room temperature) medicine as soon as possible after drawing it up. However, the medicine can remain in the syringe for up to 2 hours before injecting. If the medicine remains in the syringe for more than 2 hours, the filled syringe and needle must be discarded. 3. Why do I need to inject air into the vial? Injecting 1 mL of air into the vial makes it easier to draw up the dose into the syringe. Without the air, some liquid may flow back into the vial unintentionally, leaving less medicine than intended in the syringe. 4. Why is the ventrogluteal administration approach recommended? The ventrogluteal approach, into the gluteus medius muscle, is recommended because it is located away from major nerves and blood vessels. A dorso-gluteal approach into the gluteus maximus muscle is acceptable, if preferred by the health care professional. The injection should not be administered in any other site.
14
Apretude 600 mg prolonged-release suspension for injection comes as oral solution containing 600mg. Always follow the dose your doctor or pharmacist has given you, and read the leaflet that comes with the medicine.
The active substance in Apretude 600 mg prolonged-release suspension for injection is cabotegravir.
Medicines with the same active substance, strength and form include: Vocabria 600 mg prolonged-release suspension for injection. They are interchangeable only if your prescriber or pharmacist says so.
This leaflet reproduces the patient information leaflet approved for Apretude 600 mg prolonged-release suspension for injection, as published on the electronic medicines compendium (emc). The version printed inside your medicine’s packaging is the one that applies to you.
Whether a medicine is available over the counter or on prescription only depends on its licence. Check the leaflet, or ask your pharmacist — they can tell you straight away.
The text above reproduces the patient information leaflet approved for this medicine, restructured for easier reading.
Apretude is indicated in combination with safer sex practices for pre-exposure prophylaxis (PrEP) to reduce the risk of sexually acquired HIV-1 infection in high-risk adults and adolescents, weighing at least 35 kg (see sections 4.2, 4.4 and 5.1).
Apretude should be prescribed by a healthcare professional experienced in the management of HIV PrEP.
Each injection should be administered by a healthcare professional.
Individuals must be tested for HIV-1 prior to initiating cabotegravir and at each subsequent injection of cabotegravir (see section 4.3). A combined antigen/antibody test as well as an HIV-RNA-based test should both be negative. Prescribers are advised to perform both tests, even if the result of the HIV-RNA-based test will become available after cabotegravir injection. If a combined testing strategy including both tests is not available, testing should follow local guidelines.
Prior to starting Apretude, individuals should be carefully selected to agree to the required dosing schedule and counselled about the importance of adherence to scheduled dosing visits to help reduce the risk of acquiring HIV-1 infection.
The healthcare provider and individual may decide to use cabotegravir tablets as an oral lead-in prior to the initiation of Apretude injection to assess tolerability or may proceed directly to Apretude injections (see Table 1 and Table 2 for dosing recommendations).
Posology
Oral lead-in
Refer to the oral Apretude tablet SmPC for oral lead-in information.
Injection
Initiation injections
The recommended initial dose is a single 600 mg intramuscular injection. If oral lead-in has been used, the first injection should be planned for the last day of oral lead-in or within 3 days thereafter.
One month later, a second 600 mg intramuscular injection should be administered. Individuals may be given the second 600 mg initiation injection up to 7 days before or after the scheduled dosing date.
Continuation injections – 2 months apart
After the second initiation injection, the recommended continuation injection dose in adults is a single 600 mg intramuscular injection administered every 2 months. Individuals may be given injections up to 7 days before or after the date of the scheduled injection date.
Table 1 Recommended intramuscular dosing schedule
Initiation injections (one month apart)
Continuation injections (two months apart)
Medicinal product
Direct to injection:
months 1 and 2
or
Following oral lead-in: months 2 and 3
Two months after final initiation injection and every 2 months onwards
Cabotegravir
600 mg
600 mg
Missed doses
Individuals who miss a scheduled injection visit should be reassessed to ensure resumption of PrEP remains appropriate.
If a delay of more than 7 days from a scheduled injection date cannot be avoided, it will be a missed dose, therefore, cabotegravir 30 mg tablets may be used once daily, for a duration of up to two months, to replace one scheduled injection visit. The first dose of oral cabotegravir (or an alternative oral PrEP therapy) should be taken approximately two months (+/- 7 days) after the last injection of cabotegravir. For oral PrEP durations greater than two months, an alternative PrEP regimen to oral cabotegravir is recommended.
Injection dosing should be resumed on the day oral cabotegravir dosing completes or within 3 days, thereafter, as recommended in Table 2.
Table 2 Injection dosing recommendations after missed injections or following oral cabotegravir (PrEP) to replace an injection
Missed Doses
Time since last injection
Recommendation
If second injection is missed and time since first injection is:
≤ 2 months
Administer one 600 mg injection as soon as possible and continue with the every 2 month injection dosing schedule.
> 2 months
Restart the individual on one 600 mg initiation injection, followed by a second 600 mg initiation injection one month later. Then follow the every two month injection dosing schedule.
If 3rd or subsequent injection is missed and time since prior injection is:
≤ 3 months
Administer one 600 mg injection as soon as possible and continue with the every 2 month injection dosing schedule.
> 3 months
Restart the individual on one 600 mg initiation injection, followed by a second 600 mg initiation injection one month later. Then follow the every two month injection dosing schedule.
Special populations
Elderly
No dose adjustment is required in elderly individuals. There are limited data available on the use of cabotegravir in individuals aged 65 years and over (see section 5.2).
Hepatic impairment
No dose adjustment is required in individuals with mild or moderate hepatic impairment (Child-Pugh score A or B). Cabotegravir has not been studied in individuals with severe hepatic impairment (Child-Pugh score C, [see section 5.2]). If administered in an individual with severe hepatic impairment, cabotegravir should be used with caution.
Renal impairment
No dose adjustment is required in individuals with mild (creatinine clearance ≥60 to <90 mL/min), moderate (creatinine clearance ≥30 to <60 mL/min) or severe renal impairment (creatinine clearance ≥15 to < 30 mL/min and not on dialysis [see section 5.2]). Cabotegravir has not been studied in individuals with end-stage renal disease on renal replacement therapy. As cabotegravir is greater than 99% protein bound, dialysis is not expected to alter exposures of cabotegravir. If administered in an individual on renal replacement therapy, cabotegravir should be used with caution.
Paediatric population
The safety and efficacy of cabotegravir in children and adolescents weighing less than 35 kg have not been established. No data are available.
Method of administration
For intramuscular use. Injections must be administered to the ventrogluteal (recommended as it is located away from major nerves and blood vessels) or the dorsogluteal sites.
Care should be taken to avoid inadvertent injection into a blood vessel.
Once the suspension has been drawn into the syringe, the injection should be administered as soon as possible, but may remain in the syringe for up to 2 hours. If the medicinal product remains in the syringe for more than 2 hours, the filled syringe and needle must be discarded.
When administering Apretude injection, healthcare professionals should take into consideration the Body Mass Index (BMI) of the individual to ensure that the needle length is sufficient to reach the gluteus muscle.
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.
Individuals with an unknown or positive HIV-1 status (see sections 4.2 and 4.4).
Concomitant use with rifampicin, rifapentine, carbamazepine, oxcarbazepine, phenytoin or phenobarbital (see section 4.5).
Overall HIV-1 infection prevention strategy
Apretude may not always be effective in preventing HIV-1 infection (see section 5.1). Cabotegravir concentrations associated with significant antiviral activity (> 4x Protein Adjusted-Inhibitory Concentration, PA-IC90, see section 5.2) are achieved and maintained within hours after initiation of oral lead-in and within 7 days from the first injection (without oral lead-in). The exact time from initiation of Apretude for HIV-1 PrEP to maximal protection against HIV-1 infection is unknown.
Apretude should be used for PrEP as part of an overall HIV-1 infection prevention strategy including the use of other HIV-1 prevention measures (e.g. knowledge of HIV-1 status, regular testing for other sexually transmitted infections, condom use).
Apretude should only be used to reduce the risk of acquiring HIV-1 in individuals confirmed to be HIV negative (see section 4.3). Individuals should be re-confirmed to be HIV negative at each subsequent injection of Apretude. A combined antigen/antibody test as well as an HIV-RNA-based test should both be negative. Prescribers are advised to perform both tests, even if the result of the HIV-RNA-based test will become available after cabotegravir injection. If a combined testing strategy including both tests is not available, testing should follow local guidelines while taking Apretude.
If clinical symptoms consistent with acute viral infection are present and recent (< 1 month) exposures to HIV-1 are suspected, HIV-1 status should be reconfirmed.
Potential risk of resistance
There is a potential risk of developing resistance to cabotegravir if an individual acquires HIV-1 either before or while taking Apretude, or following discontinuation of Apretude (see Long- acting properties of Apretude injection). To minimise this risk, it is essential to confirm HIV-1 negative status at each subsequent injection of Apretude. A combined antigen/antibody test as well as an HIV-RNA-based test should both be negative. Prescribers are advised to perform both tests, even if the result of the HIV-RNA-based test will become available after cabotegravir injection. If a combined testing strategy including both tests is not available, testing should follow local guidelines.
Individuals who are diagnosed with HIV-1 should immediately begin anti-retroviral therapy (ART).
Apretude alone does not constitute a complete regimen for the treatment of HIV-1 and HIV-1 resistance mutations have emerged in some individuals with undetected HIV-1 infection who were only taking Apretude.
Importance of adherence
Individuals should be counselled periodically to strictly adhere to the recommended oral lead-in and injection dosing schedule in order to reduce the risk of HIV-1 infection and the potential development of resistance.
Long-acting properties of Apretude injection
Residual concentrations of cabotegravir may remain in the systemic circulation of individuals for prolonged periods (up to 12 months or longer), therefore, the prolonged release characteristics of Apretude injection should be taken into consideration when the medicinal product is discontinued and alternative not long-acting forms of PrEP are taken, as long as or at any time the risk of acquiring HIV is present in the months after discontinuation of Apretude (see section 5.2).
Healthcare professionals should discuss the benefit-risk of using Apretude with individuals of childbearing potential or during pregnancy (see section 4.6).
Hypersensitivity reactions
Hypersensitivity reactions have been reported in association with integrase inhibitors including cabotegravir. These reactions were characterised by rash, constitutional findings and sometimes organ dysfunction, including liver injury. Apretude and other suspected medicinal products should be discontinued immediately, should signs or symptoms of hypersensitivity develop (including, but not limited to, severe rash, or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, facial oedema, hepatitis, eosinophilia or angioedema). Clinical status, including liver aminotransferases should be monitored and appropriate therapy initiated (see sections 4.2, Long-acting properties of Apretude injection and 4.8).
Hepatoxicity
Hepatotoxicity has been reported in a limited number of individuals receiving cabotegravir with or without known pre-existing hepatic disease (see section 4.8). Administration of cabotegravir oral lead-in was used in clinical studies to help identify individuals who may be at risk of hepatotoxicity.
Clinical and laboratory monitoring are recommended and Apretude should be discontinued if hepatotoxicity is confirmed, and individuals managed as clinically indicated (see Long-acting properties of Apretude injection).
Adolescents
Suicidal ideation and suicide attempt have been reported with cabotegravir, particularly in those with pre-existing psychiatric illness (see section 4.8). Although clinical studies did not show an increased incidence of psychiatric illness in adolescents compared to adult subjects, given the vulnerability of the adolescent population, adolescents should be counselled before prescribing, and periodically while receiving Apretude, and managed as clinically indicated.
Interactions with medicinal products
Caution should be given to prescribing Apretude injection with medicinal products that may reduce its exposure (see section 4.5).
Effect of other medicinal products on the pharmacokinetics of cabotegravir
Cabotegravir is primarily metabolised by uridine diphosphate glucuronosyl transferase (UGT) 1A1 and to a lesser extent by UGT1A9. Medicinal products which are strong inducers of UGT1A1 or UGT1A9 are expected to decrease cabotegravir plasma concentrations leading to lack of efficacy (see section 4.3 and Table 3 below). In poor metabolisers of UGT1A1, representing a maximum clinical UGT1A1 inhibition, the mean AUC, Cmax and Ctau of oral cabotegravir increased by up to 1.5-fold. No dosing adjustments for Apretude are recommended in the presence of UGT1A1 inhibitors.
Cabotegravir is a substrate of P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP), however, because of its high permeability, no alteration in absorption is expected when co-administered with either P-gp or BCRP inhibitors.
Effect of cabotegravir on the pharmacokinetics of other medicinal products
In vivo, cabotegravir did not have an effect on midazolam, a cytochrome P450 (CYP) 3A4 probe. In vitro, cabotegravir did not induce CYP1A2, CYP2B6, or CYP3A4.
In vitro cabotegravir inhibited organic anion transporters (OAT) 1 (IC50=0.81 µM) and OAT3 (IC50=0.41 µM). Therefore, caution is advised when co-dosing with narrow therapeutic index OAT1/3 substrate medicinal products (e.g. methotrexate).
Based on the in vitro and clinical drug interaction profile, cabotegravir is not expected to alter concentrations of other anti-retroviral medicinal products including protease inhibitors, nucleoside reverse transcriptase inhibitors, non-nucleoside reverse transcriptase inhibitors, integrase inhibitors, entry inhibitors, and ibalizumab.
No drug interaction studies have been performed with cabotegravir injection. The drug interaction data provided in Table 3 is obtained from studies with oral cabotegravir (increase is indicated as “↑”, decrease as “↓”, no change as “↔”, area under the concentration versus time curve as “AUC”, maximum observed concentration as “Cmax”, concentration at end of dosing interval as “C”).
Table 3 Drug interactions
Medicinal products by therapeutic areas
Interaction
Geometric mean change (%)
Recommendations concerning co‑administration
HIV-1 Antiviral medicinal products
Non-nucleoside Reverse Transcriptase Inhibitor:Etravirine
Cabotegravir ↔
AUC ↑ 1%
Cmax ↑ 4%
C ↔ 0%
Etravirine did not significantly change cabotegravir plasma concentration. No dose adjustment of Apretude is necessary when initiating injections following etravirine use.
Non-nucleoside Reverse Transcriptase Inhibitor:Rilpivirine
Cabotegravir ↔AUC ↑ 12%Cmax ↑ 5%C ↑ 14%
Rilpivirine ↔AUC ↓1%Cmax ↓ 4%C ↓ 8%
Rilpivirine did not significantly change cabotegravir plasma concentration or vice versa. No dose adjustment of Apretude or rilpivirine is necessary when co-administered.
Anticonvulsants
CarbamazepineOxcarbazepinePhenytoinPhenobarbital
Cabotegravir ↓
Metabolic inducers may significantly decrease cabotegravir plasma concentration. Concomitant use is contraindicated (see section 4.3).
Antimycobacterials
Rifampicin
Cabotegravir ↓AUC ↓ 59%Cmax ↓ 6%
Rifampicin significantly decreased cabotegravir plasma concentration which is likely to result in loss of therapeutic effect. Dosing recommendations for co-administration of Apretude with rifampicin have not been established and co-administration of Apretude with rifampicin is contraindicated (see section 4.3).
Rifapentine
Cabotegravir ↓
Rifapentine may significantly decrease cabotegravir plasma concentrations. Concomitant use is contraindicated (see section 4.3).
Rifabutin
Cabotegravir ↓AUC ↓ 21%Cmax ↓ 17%
C ↓ 26%
When rifabutin is started before or concomitantly with the first cabotegravir initiation injection the recommended cabotegravir dosing schedule is one 600 mg injection followed 2 weeks later by a second 600 mg initiation injection and monthly, thereafter, while on rifabutin.
When rifabutin is started at the time of the second initiation injection or later, the recommended dosing schedule is 600 mg, monthly, while on rifabutin.
After stopping rifabutin, the recommended cabotegravir dosing schedule is 600 mg every 2 months.
Oral contraceptives
Ethinyl estradiol (EE) and Levonorgestrel (LNG)
EE ↔
AUC ↑ 2%Cmax ↓ 8%
C ↔ 0%
LNG ↔
AUC ↑ 12%Cmax ↑ 5%
C ↑ 7%
Cabotegravir did not significantly change ethinyl estradiol and levonorgestrel plasma concentrations to a clinically relevant extent. No dose adjustment of oral contraceptives is necessary when co-administered with Apretude.
Paediatric population
Interaction studies have only been performed in adults.
Women of childbearing potential
Women of childbearing potential should be counselled about prolonged release characteristics of cabotegravir injection. If a woman plans a pregnancy, the benefits and the risks of starting/continuing PrEP with Apretude should be discussed (see section 4.4).
Pregnancy
There are limited data from the use of cabotegravir in pregnant women. The effect of cabotegravir on pregnancy is unknown.
Cabotegravir was not teratogenic when studied in pregnant rats and rabbits but exposures higher than the therapeutic dose showed reproductive toxicity in animals (see section 5.3). The relevance to human pregnancy is unknown.
Apretude injection is not recommended during pregnancy unless the expected benefit justifies the potential risk to the foetus.
Cabotegravir has been detected in systemic circulation for up to 12 months or longer after an injection, therefore, consideration should be given to the potential for foetal exposure during pregnancy (see section 4.4).
Breast-feeding
It is expected that cabotegravir will be secreted into human milk based on animal data, although this has not been confirmed in humans. Cabotegravir may be present in human milk for up to 12 months or longer after the last Apretude injection.
It is recommended that women breast-feed only if the expected benefit justifies the potential risk to the infant.
Fertility
There are no data on the effects of cabotegravir on human male or female fertility. Animal studies indicate no effects of cabotegravir on male or female fertility (see section 5.3).
Individuals should be informed that dizziness, somnolence and fatigue have been reported during treatment with Apretude injection. The clinical status of the individual and the adverse reaction profile of Apretude injection should be borne in mind when considering the individual's ability to drive or operate machinery.
Summary of the safety profile
The most frequently reported adverse reactions in HPTN 083 were: Injection site reactions (82%), headache (17%) and diarrhoea (14%).
The most frequently reported adverse reactions in HPTN 084 were: Injection site reactions (38%), headache (23%) and transaminase increased (19%).
Tabulated list of adverse reactions
Adverse reactions for cabotegravir were identified from the Phase III clinical studies; HPTN 083 and HPTN 084; and post-marketing data. In HPTN 083, the median time on blinded study product was 65 weeks and 2 days (1 day to 156 weeks and 1 day), with a total exposure on cabotegravir of 3270 person years. In HPTN 084, the median time on blinded study product was 64 weeks and 1 day (1 day to 153 weeks and 1 day), with a total exposure on cabotegravir of 1920 person years.
The adverse reactions considered at least possibly related to cabotegravir in adults and adolescents are listed in Table 4 by system organ class and frequency. Frequencies are defined as very common (≥ 1/10), common (≥ 1/100 to < 1/10), uncommon (≥ 1/1 000 to < 1/100), rare (≥ 1/10 000 to < 1/1 000), very rare (< 1/10 000).
Table 4 Tabulated list of adverse reactions1
MedDRA System organ class (SOC)
Frequency category
Adverse reactions
Immune system disorders
Uncommon
Hypersensitivity*6
Psychiatric disorders
Common
Abnormal dreams
Insomnia
Depression
Anxiety
Uncommon
Suicide attempt6; Suicidal ideation6 (particularly in individuals with a pre-existing psychiatric illness)
Nervous system disorders
Very common
Headache
Common
Dizziness
Uncommon
Somnolence
Vasovagal reactions (in response to injections)
Gastrointestinal disorders
Very common
Diarrhoea
Common
Nausea
Abdominal pain2
Flatulence
Vomiting
Hepatobiliary Disorders
Uncommon
Hepatotoxicity
Skin and subcutaneous tissue disorders
Common
Rash3
Uncommon
Urticaria*6
Angioedema*6
Very rare
Stevens-Johnson syndrome*6, toxic epidermal necrolysis*6
Musculoskeletal and connective tissue disorders
Common
Myalgia
General disorders and administrative site conditions
Very common
Pyrexia5
Injection site reactions4 (pain and tenderness, nodule, induration)
Common
Injection site reaction4 (swelling, bruising, erythema, warmth, pruritus, anaesthesia)
Fatigue
Malaise
Uncommon
Injection site reactions4 (haematoma, discolouration, abscess)
Investigations
Very common
Transaminase increased
Uncommon
Weight increased
Blood bilirubin increased
1 The frequency of the identified adverse reactions are based on all reported occurrences of the adverse reactions and are not limited to those considered at least possibly related by the investigator.
2Abdominal pain includes the following grouped MedDRA preferred terms: upper abdominal pain and abdominal pain.
3Rash includes the following grouped MedDRA preferred terms: rash, rash erythematous, rash macular, rash maculo-papular, rash morbilliform, rash papular, rash pruritic.
4ISRs listed in the table have been seen in 2 participants or more.
5Pyrexia includes the following grouped MedDRA preferred terms: pyrexia and feeling hot. The majority of pyrexia adverse reactions were reported within one week of injections.
6This adverse reaction was identified through post-marketing reporting. The frequency category is based on individuals exposed to cabotegravir in clinical studies.
*Please refer to section 4.4 'Hypersensitivity reactions'.
Description of selected adverse reactions
Local injection site reactions (ISRs)
In HPTN 083, 2% of participants discontinued cabotegravir because of ISRs. Out of 20286 injections, 8900 ISRs were reported. A total of 2117 participants received at least one injection. Of the 1740 (82%) participants who experienced at least one ISR, the maximum severity of ISRs reported was mild (Grade 1, 34% of participants), moderate (Grade 2, 46% of participants) or severe (Grade 3, 3% of participants). The median duration of overall ISR adverse reactions was 4 days. The proportion of participants reporting ISRs at each visit and the severity of the ISRs decreased over time.
In HPTN 084, no participants discontinued cabotegravir because of ISRs. Out of 13068 injections, 1171 ISRs were reported. A total of 1519 participants received at least one injection. Of the 578 (38%) participants who experienced at last one ISR, the maximum severity of ISRs reported was mild (Grade 1, 25% of participants), moderate (Grade 2, 13% of participants) or severe (Grade 3, < 1% of participants). The median duration of overall ISR adverse reactions was 8 days. The proportion of participants reporting ISRs at each visit and the severity of the ISRs generally decreased over time.
Weight increased
At the week 41 and week 97 timepoints in HPTN 083, participants who received cabotegravir gained a median of 1.2 kg (Interquartile Range [IQR] -1.0, 3.5; n=1623) and 2.1 kg (IQR; -0.9, 5.9 n=601) in weight from baseline, respectively; those in the tenofovir disoproxil fumarate (TDF)/emtricitabine (FTC) group gained a median of 0.0 kg (IQR -2.1, 2.4, n=1611) and 1.0 kg (IQR; -1.9, 4.0 n=598) in weight from baseline, respectively.
At the Week 41 and Week 97 timepoints in HPTN 084, participants who received cabotegravir gained a median of 2.0 kg (IQR 0.0, 5.0; n=1151) and 4.0 kg (IQR; 0.0, 8.0, n=216) in weight from baseline, respectively; those in the tenofovir disoproxil fumarate (TDF)/emtricitabine (FTC) group gained a median of 1.0 kg (IQR -1.0, 4.0, n=1131) and 3.0 kg (IQR; -1.0, 6.0 n=218) in weight from baseline, respectively.
Changes in laboratory chemistries
In both HPTN 083 and HPTN 084, a similar proportion of participants in the cabotegravir and TDF/FTC groups were observed to have elevated hepatic transaminases (ALT/AST) levels and maximum post baseline increases were mostly Grades 1 and 2. In HPTN 083, the number of participants in the cabotegravir vs TDF/FTC groups who experienced maximum post baseline Grade 3 or 4 ALT levels were 40 (2%) vs 44 (2%) and Grade 3 or 4 AST levels were 68 (3%) vs 79 (3%), respectively. In HPTN 084, the number of participants in the cabotegravir vs TDF/FTC groups who experienced maximum post baseline Grade 3 or 4 ALT levels were 12 (< 1%) vs 18 (1%) and Grade 3 and 4 AST levels were 15 (< 1%) vs 14 (< 1%), respectively.
A few participants in both the cabotegravir and TDF/FTC groups had adverse reactions of AST or ALT increased which resulted in discontinuation of study product. In HPTN 083, the number of participants in the cabotegravir vs TDF/FTC groups who discontinued due to ALT increased were: 29 (1%) vs 31 (1%) and due to AST increased were 7 (< 1%) vs 8 (< 1%), respectively. In HPTN 084, the number of participants in the cabotegravir vs TDF/FTC groups who discontinued due to ALT increased were 12 (< 1%) vs 15 (< 1%) and there were no discontinuations due to AST increased.
Adolescents
Based on data from two open-label multicenter clinical trials (HPTN 083-01 and HPTN 084-01) in 64 HIV-uninfected, at-risk adolescents (weighing ≥ 35 kg at enrolment) receiving cabotegravir, no new safety issues were identified in adolescents compared with the safety profile established in adults receiving cabotegravir for HIV-1 PrEP in studies HPTN 083 and HPTN 084.
Based on data from the Week 16 analysis of the MOCHA study in HIV-infected adolescents (aged at least 12 years and weighing ≥35 kg) receiving background combination anti retroviral therapy, no new safety concerns were identified in adolescents with the addition of oral cabotegravir followed by injectable cabotegravir (n=29) when compared with the safety profile established with cabotegravir in adults (see section 5.1).
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation 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 via Yellow Card Scheme Website: www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store.
There is no specific treatment for Apretude overdose. If overdose occurs, the individual should be treated supportively with appropriate monitoring as necessary.
Cabotegravir is known to be highly protein bound in plasma; therefore, dialysis is unlikely to be helpful in removal of medicinal product from the body. Management of overdose with Apretude injection should take into consideration the prolonged exposure to the medicinal product following an injection (see section 4.4).
Ask anything about Apretude 600 mg prolonged-release suspension for injection. The assistant answers only from this leaflet — if the leaflet does not cover it, it will say so. It does not give medical advice.
Answers come from the patient leaflet published on the electronic medicines compendium (emc). They are not medical advice. Ask a pharmacist or your GP if you are unsure. For urgent help call NHS 111, or 999 in an emergency.
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