Active Ingredient: Rilpivirine
Rilpivirine is indicated, in combination with cabotegravir injection, for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults and adolescents (at least 12 years of age and weighing at least 35 kg) who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral regimen without present or past evidence of viral resistance to, and no prior virological failure with, agents of the non-nucleoside reverse transcriptase inhibitor (NNRTI) and integrase inhibitor (INI) class.
For this indication, competent medicine agencies globally authorize below treatments:
For:
Regimen A, in case that patient weight is ≥ 35 kg
Intramuscular, 900 milligrams rilpivirine, one dose, over the duration of 1 month. Afterwards, intramuscular, 600 milligrams rilpivirine, once monthly.
Regimen B, in case that patient weight is ≥ 35 kg
Intramuscular, 900 milligrams rilpivirine, one dose, over the duration of 1 month. Afterwards, intramuscular, 900 milligrams rilpivirine, one dose, over the duration of 2 months. Afterwards, intramuscular, 900 milligrams rilpivirine, once every 2 months.
Regimen C, in case that patient weight is ≥ 35 kg
Oral, 25 milligrams rilpivirine, once daily, over the duration of 28 days. Afterwards, intramuscular, 900 milligrams rilpivirine, one dose, over the duration of 1 month. Afterwards, intramuscular, 600 milligrams rilpivirine, once monthly.
Regimen D, in case that patient weight is ≥ 35 kg
Oral, 25 milligrams rilpivirine, once daily, over the duration of 28 days. Afterwards, intramuscular, 900 milligrams rilpivirine, one dose, over the duration of 1 month. Afterwards, intramuscular, 900 milligrams rilpivirine, one dose, over the duration of 2 months. Afterwards, intramuscular, 900 milligrams rilpivirine, once every 2 months.
Rilpivirine injection may be initiated with oral lead-in or without (direct to injection).
The healthcare professional and patient may decide to use rilpivirine tablets as an oral lead-in prior to the initiation of rilpivirine injections to assess tolerability (see Table 1), or proceed directly to rilpivirine therapy (see Tables 2 and 3, for monthly and every 2 months dosing recommendations, respectively).
When used for oral lead-in prior to the initiation of rilpivirine injection, rilpivirine oral tablets, together with cabotegravir oral tablets, should be taken for approximately 1 month (at least 28 days) to assess tolerability to rilpivirine and cabotegravir. One rilpivirine 25-mg tablet should be taken with a meal with one cabotegravir 30-mg tablet once daily (see Table 1).
Table 1. Oral Lead-in Dosing Schedule:
| Oral Lead-In | |
|---|---|
| Drug | For one month (at least 28 days), followed by the Initiation Injectiona |
| Rilpivirine | 25 mg once daily with a meal |
| Cabotegravir | 30 mg once daily |
a see Table 2 for monthly injection dosing schedule and Table 3 for every 2 months injection dosing schedule.
Initiation injection (900 mg):
On the final day of current antiretroviral therapy or oral lead-in, the recommended initiation injection dose of rilpivirine is a single 900 mg intramuscular injection.
Continuation injection (600 mg):
After the initiation injection, the recommended continuation injection dose of rilpivirine is a single 600 mg monthly intramuscular injection. Patients may be given injections up to 7 days before or after the date of the monthly injection schedule.
Table 2. Recommended monthly intramuscular injection dosing schedule:
| Medicinal Product | Initiation injection | Continuation injections |
|---|---|---|
| Initiate injection on the last day of either current ART therapy or oral lead-in (if used) | One month after initiation injection and monthly onwards | |
| Rilpivirine | 900 mg | 600 mg |
| Cabotegravir | 600 mg | 400 mg |
Initiation Injections – 1 month apart (900 mg):
On the final day of current antiretroviral therapy or oral lead-in, the recommended initial rilpivirine injection dose is a single 900 mg intramuscular injection.
One month later, a second 900 mg intramuscular injection should be administered. Patients may be given the second 900 mg injection up to 7 days before or after the scheduled dosing date.
Continuation Injections – 2 months apart (900 mg):
After the initiation injections, the recommended rilpivirine continuation injection dose is a single 900 mg intramuscular injection administered every 2 months. Patients may be given injections up to 7 days before or after the date of the every 2 months injection schedule.
Table 3. Recommended every 2 months intramuscular injection dosing schedule:
| Initiation injections | Continuation injections | |
|---|---|---|
| Medicinal Product | Initiate injection on the last day of either current ART therapy or oral lead-in (if used). One month later, a second initiation injection should be administered. | Two months after last initiation injection and every 2 months onwards |
| Rilpivirine | 900 mg | 900 mg |
| Cabotegravir | 600 mg | 600 mg |
Patients switching from a monthly continuation injection schedule to an every 2 months continuation injection schedule should receive a single 900 mg intramuscular injection of rilpivirine one month after the last 600 mg rilpivirine continuation injection dose and then 900 mg every 2 months thereafter.
Patients switching from an every 2 months continuation injection schedule to a monthly continuation injection schedule should receive a single 600 mg intramuscular injection of rilpivirine two months after the last 900 mg rilpivirine continuation injection dose and then 600 mg monthly thereafter.
Patients who miss an injection visit should be clinically reassessed to ensure resumption of therapy is appropriate. See Table 4 and 5 for dosing recommendations after a missed injection.
If a patient plans to miss a scheduled injection by more than 7 days, daily oral therapy (one rilpivirine tablet [25 mg] and one cabotegravir tablet [30 mg]) may be used to replace up to 2 consecutive monthly injection visits. Limited data is available on oral bridging with other fully suppressive antiretroviral therapy (ART) (mainly INI-based), see section 5.1.
The first dose of oral therapy should be taken 1 month (± 7 days) after the last injection doses of rilpivirine and cabotegravir. Injection dosing should be resumed on the day oral dosing completes, as recommended in Table 4.
In case more than two months need to be covered for, i.e., missing more than two monthly injections, an alternative oral regimen should be initiated one month (± 7 days) after the final injection of rilpivirine.
Table 4. Rilpivirine dosing recommendations after missed injections or oral therapy for patients on monthly injection dosing:
| Time since last injection | Recommendation |
|---|---|
| ≤2 months: | Continue with the monthly 600 mg injection schedule as soon as possible. |
| >2 months: | Re-initiate the patient on the 900 mg dose, and then continue to follow the monthly 600 mg injection schedule. |
If a patient plans to miss a scheduled injection visit by more than 7 days, daily oral therapy (one rilpivirine tablet [25 mg] and one cabotegravir tablet [30 mg]) may be used to replace one 'every 2 months' injection visit. Limited data is available on oral bridging with other fully suppressive ART (mainly INI-based).
The first dose of oral therapy should be taken approximately two months (±7 days) after the last injection doses of rilpivirine and cabotegravir. Injection dosing should be resumed on the day oral dosing completes, as recommended in Table 5.
In case more than two months need to be covered for, i.e., missing more than one 'every 2 months' injection, an alternative oral regimen should be initiated two months (± 7 days) after the final injection of rilpivirine.
Table 5. Rilpivirine dosing recommendations after missed injections or oral therapy for patients on every 2 months injection dosing:
| Missed Injection Visit | Time since last injection | Recommendation |
|---|---|---|
| Injection 2 | ≤2 months | Continue with the 900 mg injection as soon as possible and continue with every 2 months injection schedule. |
| >2 months | Re-initiate the patient on the 900 mg dose, followed by a second 900 mg initiation injection one month later. Then follow the every 2 months injection schedule. | |
| Injection 3 or later | ≤3 months | Continue with the 900 mg injection as soon as possible and continue with every 2 months injection schedule. |
| >3 months | Re-initiate the patient on the 900 mg dose, followed by a second 900 mg initiation injection one month later. Then follow the every 2 months injection schedule. |
There is limited information regarding the use of rilpivirine in patients >65 years of age. No dose adjustment of rilpivirine is required in older patients.
Care should be taken to avoid inadvertent injection of rilpivirine into a blood vessel. The suspension should be injected slowly.
Rilpivirine injection should be administered by a healthcare professional.
Rilpivirine injection should always be co-administered with a cabotegravir injection. Rilpivirine and cabotegravir injections should be administered at separate gluteal injection sites during the same visit. The order of injections is not important.
When administering rilpivirine, the healthcare professional should take into consideration the body mass index (BMI) of the patient to ensure that the needle length is sufficient to reach the gluteus muscle.
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