How effective is Roflumilast treatment? Is there anything to pay attention to when patients stop taking medication?
1、 Drug name
Common name: Repotrectinib
Product Name: AUGTYRO ™
2、 Indications
Used to treat adult patients with locally advanced or metastatic ROS1 positive non-small cell lung cancer (NSCLC).
3、 Specifications and characteristics
Specification: Capsules, each containing 40 milligrams of riptinib.
Appearance: White opaque hard shell capsule, containing white to off white powder, possibly in the form of a plug. The capsule cap is printed with the blue word 'REP40'.
4、 Main components
Active ingredient: Riptinib.
Non active ingredients: microcrystalline cellulose, sodium dodecyl sulfate, cross-linked carboxymethyl cellulose sodium, colloidal silica. The capsule shell contains gelatin and titanium dioxide. The printing ink contains insect glue and FD&C Blue No.2 aluminum lake.
5、 Usage and dosage
Recommended dosage: Oral, once daily, 160mg each time, with or without meals, taken continuously for 14 days; Afterwards, the dosage was increased to twice a day, 160 milligrams each time, until disease progression or unacceptable toxicity occurred.
Usage: Take approximately at the same time every day. The capsule should be swallowed whole and should not be opened, chewed, crushed, or dissolved. Do not take any broken, cracked or damaged capsules.
Omission or vomiting treatment: If a dose is missed or vomiting occurs at any time after taking the medication, the dose should be skipped and the next dose should be taken at the scheduled time. Should not be supplemented.
6、 Dose adjustment
According to the severity of adverse reactions, dosage adjustments may be necessary, including suspension of administration, reduction of dosage, or permanent discontinuation. The specific adjustment plan is as follows:
Central nervous system adverse reactions: In the event of intolerable grade 2 or 3 events, administration is suspended until it returns to ≤ grade 1 or baseline level, and then resumed at the same or reduced dose. When a level 4 event occurs, permanently discontinue medication.
Interstitial lung disease/pneumonia: Discontinue medication when suspected; Permanently discontinue medication after diagnosis.
Hepatotoxicity: Depending on the severity of elevated transaminase and bilirubin levels, administration is suspended until recovery, and then resumed at the same or reduced dose, or permanently discontinued. For example, when ALT or AST is greater than 3 times the upper limit of normal (ULN) and total bilirubin is greater than 1.5 times ULN, permanent discontinuation of medication is required.
Muscle pain accompanied by elevated creatine kinase: When CPK increases by more than 5 times ULN, administration is suspended until it returns to baseline or ≤ 2.5 times ULN, and then restored at the same dose; When the increase in CPK is greater than 10 times the ULN or the second occurrence of CPK is greater than 5 times the ULN, the administration is suspended until recovery, and then restored at a reduced dose.
Hyperuricemia: When a grade 3 or 4 event occurs, medication should be suspended until symptoms improve, and then restored at the same or reduced dose.
Other clinically relevant adverse reactions: In the event of intolerable grade 2 or 3 events, medication should be suspended until recovery to ≤ grade 1 or baseline. If remission occurs within 4 weeks, the same or reduced dose should be used for recovery; If there is no relief within 4 weeks, the medication will be permanently discontinued. When a level 4 event occurs, permanently discontinue medication; If it is a recurrent level 4 event, permanent discontinuation of medication is also required.
Specific reduction plan: Reduce for the first time to 120mg once daily or 120mg twice daily; Reduce the dosage for the second time to 80 milligrams once daily or twice daily.
7、 Medication precautions
Dosage: Take at approximately the same time each day, with or without food.
Swallowing method: The entire capsule must be swallowed without damaging it.
Missed dose/vomiting: skip this dose and take the next dose according to the original plan. Do not supplement or double the dose.
Dietary precautions: During treatment, avoid consuming grapefruit or drinking grapefruit juice as it may increase the blood concentration of riptinib.
Activity precautions: If there are adverse reactions to the central nervous system such as dizziness, blurred vision, balance disorders, cognitive impairment, etc., driving or operating machinery should be avoided until the symptoms are relieved.
8、 Medication for special populations
Elderly patients (≥ 65 years old): There is no clinically significant difference in safety and efficacy compared to younger patients.
Patients with renal insufficiency: Mild or moderate renal insufficiency patients do not require dose adjustment. The recommended dosage for patients with severe renal insufficiency or renal failure has not yet been determined.
Patients with liver dysfunction: Mild liver dysfunction patients do not need to adjust the dosage. The recommended dosage for patients with moderate or severe liver dysfunction has not yet been determined.
Pregnant women: may cause harm to the fetus. Pregnant women should be informed of potential risks to the fetus. Women with fertility should undergo a pregnancy test before starting treatment.
Women with fertility: During treatment and within 2 months after the last dose, effective non hormonal contraceptive measures should be taken, as riptinib may render certain hormonal contraceptives ineffective.
Male partners of women with fertility: Effective contraceptive measures should be taken during treatment and within 4 months after the last dose.
Breastfeeding women: It is recommended not to breastfeed during the treatment period and within 10 days after the last dose.
Children: The safety and efficacy of ROS1 positive NSCLC in pediatric patients have not been determined.
9、 Adverse reactions
The most common adverse reactions (≥ 20%) are dizziness, taste disorders, peripheral neuropathy, constipation, dyspnea, ataxia, fatigue, cognitive impairment, muscle weakness, and nausea.
Serious Warning and Precautions:
Central nervous system effects: including dizziness, ataxia, cognitive impairment, emotional disorders, sleep disorders, etc.
Interstitial lung disease/pneumonia.
Hepatotoxicity: Regular monitoring of liver function is necessary.
Muscle pain accompanied by elevated creatine kinase levels.
Hyperuricemia: Blood uric acid levels need to be monitored.
Bone fracture.
Embryo fetal toxicity.
10、 Contraindications
None.
11、 Drug interactions
Should avoid using:
Strong or moderate CYP3A inhibitors (such as itraconazole).
P-gp inhibitors.
Strong or moderate CYP3A inducers (such as rifampicin).
Some CYP3A substrate drugs with narrow therapeutic windows (as riptinib may lower its blood drug concentration, which may affect efficacy).
Hormonal contraceptives (which may cause contraceptive failure).
Caution should be exercised when combining with other medications: healthcare providers should be informed of all medications being used.
12、 Storage method
Store at 20 ° C to 25 ° C (68 ° F to 77 ° F); Allow short distance transportation between 15 ° C and 30 ° C (59 ° F and 86 ° F).
13、 Manufacturer
Distributed by Bristol Myers Squibb Company.
Disclaimer：《How effective is Roflumilast treatment? Is there anything to pay attention to when patients stop taking medication?》Edited and sorted by Seagull Pharmacy's editors. Please contact us in time if there is any infringement. In addition, the suggestions for drug usage, dosage and disease mentioned in the article are only for medical staff's reference, and can not be used as any basis for medication！