Javlor® [Vinflunine]
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Clinical Pharmacology
Vinflunine has a cytostatic effect associated with inhibition of tubulin polymerization during cell mitosis.
Indications
Monotherapy of adult patients with advanced or metastatic urothelial transitional cell carcinoma after treatment with platinum drugs, which did not give a positive result.
Composition
Active substance:Vinflunine 25 mg
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Dosage and Administration
IV, in the form of 6-10-minute infusion.
The drug Vinelbin is used both as monotherapy, and in combination with other anticancer drugs. When choosing a dose and mode of administration in each individual case, refer to the special literature.
In monotherapy mode, the usual dose of the drug is 25-30 mg / m2 Once a week. The drug is diluted in a 0.9% solution of sodium chloride or 5% dextrose solution to a concentration of 1.5–3 mg / ml. After the introduction of the drug, the vein should be washed, adding an additional at least 250 ml of 0.9% sodium chloride solution or 5% dextrose solution.
For patients with body surface area ≥2 m2 a single dose of the drug Vinelbin, administered IV, should not exceed 60 mg.
In polychemotherapy, the dose and frequency of administration of the drug Vinelbin depend on the specific program of antitumor therapy.
Correction of the dosing regimen of the drug Vinelbin with manifestation of hematotoxicity (depending on hematological parameters):
- when the number of neutrophils per day of administration is ≥1500 / μl, the dose does not change and amounts to 100% of the starting dose;
- when the number of neutrophils on the day of injection is 1000–
- with the number of neutrophils on the day of administration *.
Note: in patients with fever and / or sepsis on the background of neutropenia during treatment with Vinelbin or skipping 2 weekly injections of the drug in a row due to the low neutrophil content of the dose in subsequent injections should be as follows:
- when the number of neutrophils per day of administration is ≥1500 / μl, the dose is 75% of the starting dose;
- when the number of neutrophils on the day of injection is 1000–
- with the number of neutrophils on the day of administration *.
* Repeat the determination of the number of neutrophils after 1 week. When skipping 3 weekly injections of the drug in a row because of the content of neutrophils
Correction of the dosing regimen of the drug Vinelbin in liver failure:
- when the concentration of total bilirubin ≤34.2 mcmol / l, the dose does not change and is 100% of the starting dose;
- when the concentration of total bilirubin is from 35.9 to 51.3 μmol / l, the dose is 50% of the starting dose;
- when the concentration of total bilirubin is> 51.3 μmol / l, the dose is 25% of the starting dose.
Children: the safety and efficacy of Vinelbin in children has not been studied.
Older people: there are no special instructions for use of the drug Vinelbin in the elderly.
Adverse reactions
From the side of the blood system: neutropenia, anemia, thrombocytopenia. The smallest number of neutrophils is observed on the 7-10th day from the start of therapy, recovery occurs in the next 5-7 days. Cumulative hematotoxicity is not observed.
On the part of the immune system: rarely - anaphylactic shock or angioedema.
Nervous system disorders: decrease or loss of deep tendon reflexes, peripheral neuropathy (paresthesias, hyperesthesia), weakness in the legs, pain in the jaw area, severe paresthesias with sensory and motor symptoms, as a rule, are reversible.
On the part of the cardiovascular system: an increase or decrease in blood pressure, hot flushes to the face and cold extremities, coronary heart disease (angina, myocardial infarction), collapse, tachycardia, heartbeat and heart rhythm disturbances.
Respiratory system disorders: dyspnea, bronchospasm, interstitial pneumonia (with combination therapy with mitomycin), acute respiratory distress syndrome, pulmonary edema.
On the part of the digestive system: nausea, vomiting, anorexia, stomatitis, constipation, diarrhea, pancreatitis, intestinal paresis, paralytic intestinal obstruction, transient increase in bilirubin level and increased activity of hepatic transaminases.
From the skin and subcutaneous tissues: alopecia, skin rashes.
Local reactions: pain / burning or redness at the injection site, discoloration of veins, phlebitis; during extravasation - inflammation of the subcutaneous fatty tissue, possibly necrosis of the surrounding tissues.
Others: weakness, myalgia, arthralgia, fever, pain of various localization, including pain in the chest and in the area of tumor formation, hyponatremia, hemorrhagic cystitis and syndrome of inadequate secretion of ADH.
Contraindications
Carefully the drug should be prescribed for respiratory failure, inhibition of bone marrow hematopoiesis (including after previous chemotherapy or radiation treatment), hepatic and renal failure, constipation or intestinal obstruction in history, neuropathy in history, simultaneous administration of CYP3A4 isoenzyme inhibitors.
Drug interactions
When combined with other cytostatics, mutual aggravation of side effects is possible, in the first place - myelosuppression.
When combined with mitomycin, the development of acute respiratory failure.
When used in conjunction with paclitaxel, the risk of neurotoxicity increases.
Application on the background of radiation therapy leads to radiosensitization. The use of Vinelbin after radiation therapy can lead to the reappearance of radiation reactions.
The simultaneous use of the drug with inducers and inhibitors of cytochrome P450 may lead to changes in the pharmacokinetics of vinorelbine.
When used concurrently with CYP3A4 isoenzyme inhibitors, serious side effects may increase.
Pregnancy and Lactation
The drug is contraindicated in pregnancy and lactation.
During and for at least 3 months after cessation of therapy, it is necessary to use reliable methods of contraception.
Special instructions
Vinelbin treatment should be carried out under the supervision of a physician with experience in working with anticancer drugs.
Vinelbin treatment is carried out under strict hematological control, determining the number of leukocytes, neutrophils, platelets and hemoglobin level before each regular injection.
In case of severe impaired liver function, the dose of Vinelbin should be reduced depending on the concentration of total bilirubin.
In case of impaired renal function, enhanced monitoring of the patient is necessary.
Before and during treatment (before each regular injection), it is necessary to determine the activity of ALT, ACT, ALP, bilirubin concentration.
If there are signs of neurotoxicity 2nd and more degree, drug treatment should be canceled.
If dyspnea, cough or hypoxia of unknown etiology occurs, the patient should be examined to exclude pulmonary toxicity.
With extravasation, the infusion of the drug should be immediately stopped, the remaining dose is injected into another vein.
In case of contact with Vinelbin in the eyes, they should be washed thoroughly and thoroughly with water.
Overdosage
The main expected manifestations of overdose include suppression of bone marrow function and manifestations of neurotoxicity.
Treatment: symptomatic. The specific antidote is not known. In case of overdose, the patient should be hospitalized and the functions of vital organs should be carefully monitored.
- Brand name: Javlor
- Active ingredient: Vinflunine
- Dosage form: Concentrate for solution for infusion
- Manufacturer: Pierre Fabre Medicament
- Country of Origin: France
Studies and clinical trials of Vinflunine (Click to expand)
- Complete assignment of 1H and 13C NMR spectra of vinflunine
- Vinflunine in platinum-pretreated patients with locally advanced or metastatic urothelial carcinoma : Results of a large phase 2 study
- Synthesis and study of a molecularly imprinted polymer for specific solid-phase extraction of vinflunine and its metabolite from biological fluids
- Synthesis and biological evaluation of C-12′ substituted vinflunine derivatives
- Development of a sensitive liquid chromatography method coupled with a tandem mass spectrometric detection for the clinical analysis of vinflunine and 4-O-deacetyl vinflunine in blood, urine and faeces
- Reactivity of Vinca alkaloids in superacid: An access to vinflunine, a novel anticancer agent
- Determination of vinflunine in rat plasma by liquid chromatography–electrospray ionization mass spectrometry for a pharmacokinetic study
- Vinflunine, the latest Vinca alkaloid in clinical development: A review of its preclinical anticancer properties
- Pharmacokinetics, tissue distribution and excretion of vinflunine
- Cell cycle effects of vinflunine, the most recent promising Vinca alkaloid, and its interaction with radiation, in vitro
- Further mechanistic unravelling of the influence of the cell cycle effects on the radiosensitising mechanism of vinflunine, in vitro
- Preclinical in vivo antitumor activity of vinflunine, a novel fluorinated Vinca alkaloid
- In vitro synergistic effects of vinflunine, a novel fluorinated vinca alkaloid, in combination with other anticancer drugs
- Markedly diminished drug resistance-inducing properties of vinflunine (20′,20′-difluoro-3′,4′-dihydrovinorelbine) relative to vinorelbine, identified in murine and human tumour cells in vivo and in vitro
- A phase I clinical and pharmacological study evaluating vinflunine in combination with doxorubicin as first line treatment in metastatic breast cancer
- Phase I study of Vinflunine administered as a 10-minute infusion on days 1 and 8 every 3 weeks
- Phase II study of vinflunine in patients with metastatic renal cell carcinoma
- Murine leukemia P388 vinorelbine-resistant cell lines are sensitive to vinflunine
- Phase I trial of vinflunine and pemetrexed in refractory solid tumors
- A phase I evaluation of the combination of vinflunine and erlotinib in patients with refractory solid tumors
- CYP3A4 mediated in vitro metabolism of vinflunine in human liver microsomes
- CYP3A4 mediated in vitro metabolism of vinflunine in human liver microsomes
- Vinflunine – an active chemotherapy for treatment of advanced non-small-cell lung cancer previously treated with a platinum-based regimen: results of a phase II study
- A phase II study of vinflunine in bladder cancer patients progressing after first-line platinum-containing regimen