Resinib Capsule 50 mg
Resinib Capsule 50 mg Uses, Dosage, Side Effects, Food Interaction and all others data.
Resinib Capsule 50 mg inhibits cellular signaling by targeting multiple receptor tyrosine kinases (RTKs).
These include all receptors for platelet-derived growth factor (PDGF-Rs) and vascular endothelial growth factor receptors (VEGFRs), which play a role in both tumor angiogenesis and tumor cell proliferation. The simultaneous inhibition of these targets therefore reduces tumor vascularization and triggers cancer cell apoptosis and thus results in tumor shrinkage.
Resinib Capsule 50 mg also inhibits CD117 (c-KIT), the receptor tyrosine kinase that (when improperly activated by mutation) drives the majority of gastrointestinal stromal cell tumors. It has been recommended as a second-line therapy for patients whose tumors develop mutations in c-KIT that make them resistant to imatinib, or who the cannot tolerate the drug.
In addition, sunitinib binds other receptors. These include: RET, CD114, CD135. The fact that sunitinib targets many different receptors, leads to many of its side effects such as the classic hand-foot syndrome, stomatitis, and other dermatologic toxicities.
Resinib Capsule 50 mg is an oral, small-molecule, multi-targeted receptor tyrosine kinase (RTK) inhibitor that was approved by the FDA on January 26, 2006.
| Trade Name | Resinib Capsule 50 mg |
| Availability | Prescription only |
| Generic | Sunitinib |
| Sunitinib Other Names | Sunitinib, Sunitinibum |
| Related Drugs | Keytruda, pembrolizumab, fluorouracil, Avastin, imatinib, bevacizumab, Opdivo, Gleevec, gemcitabine, everolimus |
| Weight | 50 mg |
| Type | Capsule |
| Formula | C22H27FN4O2 |
| Weight | Average: 398.4738 Monoisotopic: 398.211804333 |
| Protein binding | Binding of sunitinib and its primary metabolite to human plasma protein in vitro was 95% and 90%, respectively. |
| Groups | Approved, Investigational |
| Therapeutic Class | Targeted Cancer Therapy |
| Manufacturer | Jenphar Bangladesh Ltd. |
| Available Country | Bangladesh |
| Last Updated: | October 19, 2023 at 6:27 am |
Uses
Gastrointestinal Stromal Tumor (GIST): Resinib Capsule 50 mg is used for the treatment of gastrointestinal stromal tumor after disease progression on or intolerance to imatinib mesylate.
Advanced Renal Cell Carcinoma (RCC): Resinib Capsule 50 mg is used for the treatment of advanced renal cell carcinoma.
Advanced Pancreatic Neuroendocrine Tumors (pNET): Resinib Capsule 50 mg is used for the treatment of progressive, well-differentiated pancreatic neuroendocrine tumors in patients with unresectable locally advanced or metastatic disease.
Resinib Capsule 50 mg is also used to associated treatment for these conditions: Advanced Renal Cell Carcinoma, Soft Tissue Sarcoma (STS), Thyroid Cancers, Metastatic Pancreatic Neuroendocrine Tumors, Refractory Gastrointestinal stromal tumor, Unresectable, locally advanced Pancreatic Neuroendocrine Tumors
How Resinib Capsule 50 mg works
Resinib Capsule 50 mg is a small molecule that inhibits multiple RTKs, some of which are implicated in tumor growth, pathologic angiogenesis, and metastatic progression of cancer. Resinib Capsule 50 mg was evaluated for its inhibitory activity against a variety of kinases (>80 kinases) and was identified as an inhibitor of platelet-derived growth factor receptors (PDGFRa and PDGFRb), vascular endothelial growth factor receptors (VEGFR1, VEGFR2 and VEGFR3), stem cell factor receptor (KIT), Fms-like tyrosine kinase-3 (FLT3), colony stimulating factor receptor Type 1 (CSF-1R), and the glial cell-line derived neurotrophic factor receptor (RET). Resinib Capsule 50 mg inhibition of the activity of these RTKs has been demonstrated in biochemical and cellular assays, and inhibition of function has been demonstrated in cell proliferation assays. The primary metabolite exhibits similar potency compared to sunitinib in biochemical and cellular assays.
Dosage
Resinib Capsule 50 mg dosage
Recommended Dose For GIST And RCC:The recommended dose of Resinib Capsule 50 mg for gastrointestinal stromal tumor (GIST) and advancedrenal cell carcinoma(RCC) is one 50 mg oral dose taken once daily, on a schedule of 4 weeks on treatment followed by 2 weeks off (Schedule 4/2). Resinib Capsule 50 mg may be taken with or without food.
Recommended Dose For pNET: The recommended dose of Resinib Capsule 50 mg for pancreatic neuroendocrine tumors (pNET) is 37.5 mg taken orally once daily continuously without a scheduled off-treatment period. Resinib Capsule 50 mg may be taken with or without food.
Dose Modification: Dose interruption and/or dose modification in 12.5 mg increments or decrements is recommended based on individual safety and tolerability. The maximum dose administered in the Phase 3 pNET study was 50 mg daily.
Strong CYP3A4 inhibitors such as ketoconazole may increas e sunitinib plasma concentrations. Selection of an alternate concomitant medication with no or minimal enzyme inhibition potential is recommended. A dose reduction for Resinib Capsule 50 mg to a minimum of 37.5 mg (GIST and RCC) or 25 mg (pNET) daily should be considered if Resinib Capsule 50 mg must be co-administered with a strong CYP3A4 inhibitor
CYP3A4 inducers such as rifampin may decreas e sunitinib plasma concentrations. Selection of an alternate concomitant medication with no or minimal enzyme induction potential is recommended. A dose increase for Resinib Capsule 50 mg to a maximum of 87.5 mg (GIST and RCC) or 62.5 mg (pNET) daily should be considered if Resinib Capsule 50 mg must be co-administered with a CYP3A4 inducer. If dose is increased, the patient should be monitored carefully for toxicity
Side Effects
Fatigue, GI disorders, skin discoloration, rash, palmar-plantar erythrodysesthesia, dry skin, hair color changes, mucosal inflammation, asthenia, dysguesia, anorexia, HTN, neutropenia.
Toxicity
The maximally tolerated dose for rat, mouse, and dog when given orally is greater than 500 mg/kg. The maximally tolerated dose of a non-human primate is greater 1200 mg/kg.
Interaction
Increased plasma cone with strong CYP3A4 inhibitors (eg ketoconazole, ritonavir, itraconazole, erythromycin, clarithromycin, grapefruit juice). Decreased plasma cone with strong CYP3A4 inducers [eg rifampin, dexamethasone, phenytoin, carbamazepine, phenobarb, St. John's wort (Hypericum perforatum)]. Anticoagulants eg warfarin, acenocoumarol (periodically monitor platelets, prothrombin time/INR & physical exam).
Food Interaction
- Avoid grapefruit products. Grapefruit may reduce the CYP3A4 metabolism of sunitinib.
- Avoid St. John's Wort. This herb induces CYP3A4 metabolism, which may reduce the serum concentration of sunitinib.
- Take with or without food.
[Moderate] GENERALLY AVOID: Consumption of grapefruit or grapefruit juice during sunitinib therapy may increase the plasma concentrations of sunitinib.
The proposed mechanism is inhibition of CYP450 3A4-mediated metabolism by certain compounds present in grapefruit.
MANAGEMENT: Although clinical data are lacking, it may be advisable to avoid the consumption of large amounts of grapefruit or grapefruit juice during sunitinib therapy.
Resinib Capsule 50 mg Hypertension interaction
[Moderate] The use of sunitinib has been associated with hypertension and it should be used with caution in patients with elevated blood pressure.
Therapy with sunitinib should be withheld in case of severe hypertension and appropriate measures should be taken to correct the blood pressure to acceptable readings.
Close monitoring of blood pressure is recommended.
Resinib Capsule 50 mg Drug Interaction
Major: sotalolModerate: aripiprazole, amitriptyline, heparin, levofloxacinUnknown: rabeprazole, darbepoetin alfa, torsemide, fluorouracil topical, gemcitabine, imatinib, amlodipine, phenazopyridine, bioflavonoids, metoclopramide, vitamin a topical, bioflavonoids, ampicillin / sulbactam, cyanocobalamin, cholecalciferol
Resinib Capsule 50 mg Disease Interaction
Major: liver diseaseModerate: lung toxicity, adrenal toxicity, cardiovascular Events, dermatologic toxicities, hemorrhagic events, hypertension, hypoglycemia, ONJ, proteinuria, QT prolongation, thyroid abnormality, Sunitinib – renal disease
Volume of Distribution
- 2230 L (apparent volume of distribution, Vd/F)
Elimination Route
Maximum plasma concentrations (Cmax) of sunitinib are generally observed between 6 and 12 hours (Tmax) following oral administration. Food has no effect on the bioavailability of sunitinib. Resinib Capsule 50 mg may be taken with or without food. The pharmacokinetics were similar in healthy volunteers and in the solid tumor patient populations tested, including patients with GIST and RCC.
Half Life
Following administration of a single oral dose in healthy volunteers, the terminal half-lives of sunitinib and its primary active metabolite are approximately 40 to 60 hours and 80 to 110 hours, respectively.
Clearance
- 34 - 62 L/h [Total oral clearance]
Elimination Route
Resinib Capsule 50 mg is metabolized primarily by the cytochrome P450 enzyme, CYP3A4, to produce its primary active metabolite, which is further metabolized by CYP3A4. Elimination is primarily via feces. In a human mass balance study of [14C]sunitinib, 61% of the dose was eliminated in feces, with renal elimination accounting for 16% of the administered dose.
Pregnancy & Breastfeeding use
Pregnancy Category D. There is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks.
Contraindication
Hypersensitivity, Renal impairment
Acute Overdose
Treatment of overdose with Resinib Capsule 50 mg should consist of general supportive measures. There is no specific antidote for overdosage with Resinib Capsule 50 mg. If indicated, elimination of unabsorbed drug should be achieved by emesis or gastric lavage. Cases of accidental overdose have been reported; these cases were associated with adverse reactions consistent with the known safety profile of Resinib Capsule 50 mg, or without adverse reactions. A case of intentional overdose involving the ingestion of 1,500 mg of Resinib Capsule 50 mg in an attempted suicide was reported without adverse reaction. In non-clinical studies mortality was observed following as few as 5 daily doses of 500 mg/kg (3000 mg/m²) in rats. At this dose, signs of toxicity included impaired muscle coordination, head shakes, hypoactivity, ocular discharge, piloerection and gastrointestinal distress. Mortality and similar signs of toxicity were observed at lower doses when administered for longer durations.
Innovators Monograph
You find simplified version here Resinib Capsule 50 mg
Resinib Capsule 50 mg contains Sunitinib see full prescribing information from innovator Resinib Capsule 50 mg Monograph, Resinib Capsule 50 mg MSDS, Resinib Capsule 50 mg FDA label
FAQ
What is Resinib Capsule 50 mg used for?
Resinib Capsule 50 mg Resinib Capsule 50 mg used for the treatment of renal cell carcinoma (RCC) and imatinib-resistant gastrointestinal stromal tumor (GIST).
How safe is Resinib Capsule 50 mg?
Individualised Resinib Capsule 50 mg therapy is feasible, safe and an effective method to manage toxicity with one of the best efficacy seen for oral vascular endothelial growth factor inhibitors in metastatic renal cell carcinom.
How does Resinib Capsule 50 mg work?
By blocking a particular enzyme from working, this medication can slow the growth of cancer cells.
What are the common side effects of Resinib Capsule 50 mg?
Common side effects of Resinib Capsule 50 mg are include:
- Fatigue.
- Diarrhea.
- Nausea and vomiting.
- Heartburn.
- Taste changes.
- Hypertension (high blood pressure)
- Low blood counts. ...
- Skin discoloration (possibly due to the drug color - yellow)
Is Resinib Capsule 50 mg safe during pregnancy?
Use should be avoided. If used during pregnancy or if pregnancy occurs, apprise the patient of potential hazard to the fetus. As angiogenesis is a critical component of embryonic and fetal development, this drug is expected to cause fetal harm if administered to pregnant women.
Is Resinib Capsule 50 mg safe during breastfeeding?
A decision should be made to discontinue breastfeeding or discontinue the Resinib Capsule 50 mg, taking into account the importance of the Resinib Capsule 50 mg to the mother.
Can I drink alcohol with Resinib Capsule 50 mg?
The drinking of alcohol (in small amounts) does not appear to affect the safety or usefulness of Resinib Capsule 50 mg.
How to take Resinib Capsule 50 mg?
Resinib Capsule 50 mg is usually taken once a day.Take Resinib Capsule 50 mg at around the same time every day.
How long can I take Resinib Capsule 50 mg?
Resinib Capsule 50 mg is taken once every day for 4 weeks (28 days), then it is stopped for 2 weeks (14 days). This is 1 cycle of treatment. This cycle is repeated for as long as your doctor tells you to.
How long does Resinib Capsule 50 mg stay in my system?
One dose of Resinib Capsule 50 mg takes between 8 and 12 days before most (96%) of it to leave your body. Some of the Resinib Capsule 50 mg is broken down by the body into an active metabolite which takes between 16 and 23 days for most (96%) to be removed from the body.
Does Resinib Capsule 50 mg cause hair loss?
Hair loss may not be serious but may cause concern.
Who should not take Resinib Capsule 50 mg?
Resinib Capsule 50 mg can cause severe or fatal effects on your liver. You will need frequent blood tests to check your liver function during treatment. Call your doctor if you have any signs of a liver problem, such as right-sided upper stomach pain, itching, dark urine, or jaundice (yellowing of the skin or eyes).
What happens if I miss a dose?
Use the medicine as soon as you can, but skip the missed dose if you are more than 12 hours late for the dose. Do not use two doses at one time.
Does Resinib Capsule 50 mg cause high blood pressure?
Many patients taking Resinib Capsule 50 mg experience hypertension (high blood pressure) as a side effect.
Can Resinib Capsule 50 mg cause stomach pain?
Bleeding is common with Resinib Capsule 50 mg, but can also cause severe bleeding problems that can lead to death.
Is Resinib Capsule 50 mg cytotoxic?
In pancreatic neuroendocrine tumours, sunitinib is taken continuously. Targeted therapies are not cytotoxic and do not require cytotoxic handling precautions.
Can I take overdose of Resinib Capsule 50 mg?
If you take too much Resinib Capsule 50 mg, call your healthcare provider or local Poison Control Center, or seek emergency medical attention right away.
Is there any food or drink I need to avoid when taking Resinib Capsule 50 mg?
Grapefruit and grapefruit juice may interact with Resinib Capsule 50 mg and lead to potentially dangerous effects. Discuss the use of grapefruit products with your doctor.
How is Resinib Capsule 50 mg eliminated from the body??
Resinib Capsule 50 mg is primarily eliminated with the feces , with renal elimination accounting for only 16% of the administered dose.
