LuciRip Ripretinib Tablets 50mg

Drug Name: Ripretinib Tablets

English Name: Ripretinib Tablets

Trade Names: Qinlock, LuciRip

Specification: Each tablet contains 50 mg of Ripretinib; 90 tablets per box.

Manufacturer: Lucius Pharmaceuticals Co., Ltd. (Laos)

Laos National Drug Administration Approval No.: 06L1356/25

[Indications]

Indicated for the treatment of adult patients with advanced gastrointestinal stromal tumor (GIST) who have previously received treatment with 3 or more kinase inhibitors (including imatinib).

[Dosage and Administration]

Standard Dosage

Recommended Dose: 150 mg (3 tablets of 50 mg), once daily, taken orally.

Administration Method: May be taken with or without food. Tablets should be swallowed whole; do not break, crush, or chew the tablets.

Timing: It is recommended to take the medication at the same time each day.

Dosage Adjustment

During treatment, your doctor will determine whether to temporarily interrupt dosing, reduce the dose, or permanently discontinue the medication based on your body's response to the drug and any side effects that occur.

First Dose Reduction: 100 mg (2 tablets of 50 mg), once daily.

Permanent Discontinuation: If the 100 mg once-daily dose cannot be tolerated.

Missed Dose Management

If you forget to take a dose and there are more than 8 hours remaining before your next scheduled dose, take the missed dose as soon as possible.

If there are fewer than 8 hours remaining before your next scheduled dose, skip the missed dose and take the next dose at your regularly scheduled time. Do not take a double dose to make up for a missed dose.

- If vomiting occurs after taking the medication, do not take an additional dose; simply take your next scheduled dose at the regular time.

[Use in Specific Populations]

Population Category: Precautions

Pediatric Patients: The safety and efficacy of this medication in pediatric patients have not been established.

Geriatric Patients: Studies have shown no significant differences in safety or efficacy between elderly patients and younger patients.

Patients with Renal Impairment: No dose adjustment is required for patients with mild to moderate renal impairment; due to a lack of study data, a recommended dose cannot be provided for patients with severe renal impairment. Patients with Hepatic Impairment: No dose adjustment is required for patients with mild to severe hepatic impairment; however, data for patients with severe hepatic impairment are limited, and close monitoring is recommended.

[Important Information Before Use]

Contraindications

Repatynib is contraindicated in patients with a history of severe hypersensitivity to Repatynib or to any other component of the tablet.

Important Precautions

Before starting Repatynib, please be sure to inform your doctor of your complete medical history and health conditions, particularly the following:

Skin Issues: History of Palmar-Plantar Erythrodysesthesia Syndrome (PPES, also known as hand-foot skin reaction), skin rashes, skin cancer, etc.

Hypertension: History of high blood pressure, or blood pressure that is poorly controlled.

Cardiac Issues: History of heart conditions, such as heart failure.

Planned Surgery: Repatynib may affect wound healing. If you are planning to undergo surgery (including dental surgery), you must inform your doctor. Typically, the medication must be discontinued at least one week prior to surgery and should not be resumed until at least two weeks after surgery, once the wound has completely healed.

Allergies: Inform your doctor if you have a history of allergies to other medications, foods, or additives.

Drug Interactions

Repatynib may interact with many other medications, potentially affecting its efficacy or increasing the risk of side effects. Please be sure to inform your doctor of all medications you are currently taking, including prescription drugs, over-the-counter medications, vitamins, and herbal supplements.

Specific medications to avoid or use with caution include:

Strong and Moderate CYP3A Inducers: These medications can decrease the concentration of Repatynib in the body, potentially rendering it ineffective. Examples include: rifampin, carbamazepine, phenytoin, phenobarbital, and St. John's wort (*Hypericum perforatum*).

Strong CYP3A Inhibitors: These medications can increase the concentration of Repatynib in the body, thereby increasing the risk of side effects. Examples include: certain antifungal medications (itraconazole, ketoconazole), certain antiviral medications (ritonavir), and clarithromycin.

Grapefruit or Grapefruit Juice: These should also be avoided.

[Pharmacological Action]

Mechanism of Action: A tyrosine kinase switch-control inhibitor that broadly inhibits primary and secondary mutations of KIT and PDGFRA through a dual mechanism (by modulating both the kinase switch pocket and the activation loop). Inhibition Targets: KIT (exons 9/11/13/14/17/18), PDGFRA (exons 12/14/18, including D842V); *in vitro*, it also inhibits PDGFRB, TIE2, VEGFR2, and BRAF.

【Side Effects】

Common Side Effects

Please inform your doctor if any of the following side effects occur and persist without relief or worsen:

Skin: Hair loss, dry or itchy skin, rash

Digestive System: Nausea, vomiting, diarrhea, constipation, abdominal pain, mouth sores, decreased appetite

Systemic: Fatigue, weakness, numbness or tingling sensation in the hands or feet

Musculoskeletal: Muscle or joint pain, muscle spasms

Other: Headache, weight loss

Serious Side Effects

Seek immediate medical attention if any of the following symptoms occur:

Hand-Foot Skin Reaction (PPES): Redness, swelling, pain, blistering, bleeding, or peeling of the skin on the palms of the hands or soles of the feet.

New Skin Cancer: Appearance of new warts, skin spots, or moles that change in color or size, or sores that do not heal.

High Blood Pressure: Severe headache, dizziness, blurred vision.

Symptoms of Heart Failure: Fatigue, difficulty breathing, shortness of breath when lying flat, swelling in the abdomen or legs/ankles, distended neck veins.

Severe Allergic Reaction: Rash, itching, difficulty breathing, swelling of the face/lips/tongue/throat.

Poor Wound Healing.

【Special Populations and Lifestyle Considerations】

Pregnancy and Lactation

Pregnancy: Ripretinib may cause harm to the fetus. Women of childbearing potential must undergo a pregnancy test prior to starting the medication and use effective contraception during treatment and for at least 1 week after discontinuing the drug. Male patients engaging in sexual activity with female partners of childbearing potential should also use effective contraception during treatment and for at least 1 week after discontinuing the drug. If you become pregnant while taking this medication, please inform your doctor immediately.

Lactation: Do not breastfeed during treatment and for at least 1 week after discontinuing the drug.

Effects on Male Fertility

This medication may reduce male fertility. If you are planning to conceive, please consult your doctor in advance.

Photosensitivity

Repatinib may make your skin more sensitive to sunlight. During treatment and for at least one week after discontinuing the medication, you should avoid prolonged exposure to sunlight as much as possible. When going outdoors, it is recommended to wear protective clothing, hats, and sunglasses, and to use a high-SPF sunscreen.

[Pharmacokinetics]

Absorption: Rapidly absorbed following oral administration; time to reach peak concentration is approximately 4 hours. Food has no significant effect.

Distribution: Highly protein-bound (approximately 99%); has a large apparent volume of distribution.

Metabolism: Primarily metabolized via CYP3A4; the active metabolite is DP-5439.

Excretion: Elimination half-life is approximately 14 hours; primarily excreted via feces (approximately 70%) and urine (approximately 15%).

[Storage and Disposal]

Storage: Store at room temperature (20°C–25°C), away from light, excessive heat, and moisture (do not store in the bathroom). Be sure to keep the desiccant packet inside the bottle; keep the bottle cap tightly closed after each use.

Disposal: Please dispose of expired or unwanted medication through a medication take-back program; do not flush down the toilet or discard indiscriminately.