Fostemsavir is a human immunodeficiency virus type 1 (HIV-1) gp120 targeted attachment inhibitor and belongs to the class of antiretroviral drugs.

1、 Drug name

1. Product Name: RUKOBIA

2. Common name: Fostemsavir sustained-release tablets

2、 Indications

This product, in combination with other antiretroviral drugs, is suitable for the treatment of adult patients with multidrug-resistant HIV-1 infection who have received multiple treatments in the past and have failed the current treatment plan due to drug resistance, intolerance, or safety considerations.

3、 Specifications and characteristics

1. Specification: Each tablet contains 600mg of Fosacivir (equivalent to 725mg of Fosacivir Aminobutriol).

2. Appearance: beige, oval, film coated, double convex tablet, with the words "SV1V7" engraved on one side. The pills may have a slight vinegar smell.

4、 Main components

1. Active ingredient: Fostemavir tromethamine. It is a prodrug that is converted into the active ingredient telmisavir after entering the body.

2. Non active ingredients: colloidal silica, hydroxypropyl cellulose, hydroxypropyl methylcellulose, and magnesium stearate. The film coating contains iron oxide red, iron oxide yellow, polyethylene glycol, polyvinyl alcohol, talc powder, and titanium dioxide.

5、 Usage and dosage

1. Recommended dosage: Take one tablet (600mg) twice a day, with or without meals.

2. Usage: Swallow the whole tablet. Do not chew, crush, or pry open the pills.

6、 Dose adjustment

1. Liver injury: Patients with mild to severe liver injury (Child Pugh A, B, or C grade) do not require dose adjustment.

2. Renal injury: Patients with renal injury or undergoing hemodialysis do not need to adjust the dosage.

7、 Medication precautions

1. Meal/fasting: can be taken with food or on an empty stomach. High fat meals can increase drug absorption, but there is no need to adjust the dosage accordingly.

2. Leakage treatment: If one dose is missed, it should be replenished as soon as possible. Do not take two or double doses at the same time.

3. Important reminder: Do not discontinue or cut off medication supply without authorization, as this may lead to a rebound in viral load or the development of drug resistance.

4. Pill odor: Tablets may have a slight vinegar smell, which is a normal phenomenon.

8、 Medication for special populations

1. Pregnancy: There is a registration office for exposure during pregnancy. Animal studies have not shown clinically significant developmental toxicity. At present, there is insufficient human data to determine drug-related risks.

2. Breastfeeding: It is not yet clear whether RUKOBIA is secreted through human milk. Given the risk of HIV transmission and potential serious adverse reactions associated with breastfeeding, it is recommended that women infected with HIV-1 do not breastfeed.

3. Children: The safety and efficacy in pediatric patients have not yet been determined.

4. Elderly: Limited data on patients aged 65 and above in clinical studies. Elderly patients may be more sensitive to drug-induced QT interval prolongation and should use medication with caution.

9、 Adverse reactions

1. The most common adverse reaction (incidence ≥ 5%) is nausea.

2. Common adverse reactions (incidence ≥ 2%): diarrhea, headache, abdominal pain, indigestion, fatigue, rash, sleep disorders, immune reconstitution inflammatory syndrome, drowsiness, vomiting.

3. Serious adverse reactions: immune reconstitution syndrome, prolonged QTc interval (especially when the recommended dose is exceeded), and increased liver transaminase in patients with hepatitis B or hepatitis C infection.

4. Abnormal laboratory tests: There may be abnormalities in indicators such as creatinine, bilirubin, liver enzymes, blood lipids, lipase, blood and urine glucose.

10、 Contraindications

1. It is contraindicated for individuals who are allergic to rituximab or any excipients.

2. It is prohibited to use it in combination with potent cytochrome P450 3A inducers (such as carbamazepine, rifampicin, phenytoin, enzalutamide, mitotane, St. John's wort), as it may significantly reduce the plasma concentration of telmisavir and cause virological response failure.

11、 Drug interactions

1. Strong CYP3A inducer: Do not use in combination as it significantly reduces the concentration of telmisavir (see contraindications for details).

2. Oral contraceptives: When combined with oral contraceptives containing ethinylestradiol, the concentration of ethinylestradiol increases. The daily dose of ethinylestradiol should not exceed 30mcg.

3. Statins: When used in combination with rosuvastatin, atorvastatin, etc., the concentration of statins increases, and adverse reactions should be monitored from the lowest dose.

4. Direct antiviral drugs for HCV: Combination with gezovir or fosilavir may increase their concentration and should be used with caution.

5. Medications that prolong the QT interval: When used in combination with drugs known to have a risk of apical torsion ventricular tachycardia, there may be an increased risk of arrhythmia, and caution should be exercised.

6. Other: When used in combination with Azanavir/Litonavir, Kobistat, Darunavir/Kobistat, Ittrevirine, Maravelo, etc., there is no need to adjust the dosage.

12、 Storage method

1. Store at room temperature ranging from 20 ° C to 25 ° C (68 ° F to 77 ° F); Allow brief fluctuations to 15 ° C to 30 ° C (59 ° F to 86 ° F).

2. Please keep it out of reach of children. This product is packaged to prevent children from opening it.

13、 Manufacturer

Manufacturer: ViiVHealthcare (headquartered in Durham, North Carolina, USA).

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