Vinflunine

Structural formula
General
Non-proprietary name	Vinflunine
Molecular formula	C 45 H 54 F 2 N 4 O 8
External identifiers / databases
PubChem	6918295
Wikidata	Q2195393
Drug information
ATC code	L01 CA05
Drug class	Cytostatics , vinca alkaloid - analogue
properties
Molar mass	816.92 g · mol -1
safety instructions
	Please note the exemption from the labeling requirement for drugs, medical devices, cosmetics, food and animal feed
GHS hazard labeling ; no classification available
	As far as possible and customary, SI units are used. Unless otherwise noted, the data given apply to standard conditions .

Vinflunine is a chemotherapy drug used to treat advanced cancer. The drug is a fluorinated derivative of vinorelbine and was developed by the French company Laboratoires Pierre Fabre in Castres.

indication

Vinflunine was approved by the EU Commission in 2009 under the name Javlor for the treatment of advanced or metastatic transitional cell carcinoma after failure of a first-line treatment ( M V A C or gemcitabine / cisplatin). To date, vinflunine is the only chemotherapy approved in Europe for this indication for second-line treatment. The effectiveness of vinflunine in this indication was documented for approval in two multicenter, open, single-arm phase II and one multicentre, open, controlled, randomized phase III study .

An application to the European Medicines Agency (EMA) for an additional indication for the treatment of metastatic breast cancer (breast cancer) in the case of taxane resistance failed in 2014.

Working principle

Like all vinca alkaloids, vinflunine is a spindle poison ( mitosis inhibitor / antitubulin) and hinders the formation of the so-called microtubules of the nuclear spindle, which in mitotic cell division ( anaphase / telophase ) pull the two new sets of chromosomes to the cell poles, and thus those that are uncontrolled in tumor diseases Interrupts cell division.

unwanted effects

The most common side effects seen in the studies in patients with transitional cell carcinoma of the urothelium were: blood disorders, mainly neutropenia (lack of white blood cells) and anemia (low red blood cell count); gastrointestinal disorders, especially constipation (constipation), decreased appetite ( anorexia ) and weight loss, nausea, inflammation of the mucous membranes ( stomatitis / mucositis ), vomiting, abdominal pain and diarrhea (diarrhea); general disorders such as weakness ( asthenia ) and tiredness.

Neutropenia can be controlled by administering certain drugs ( G-CSF ), but in most cases the vinflunine dose will also be adjusted. It is not uncommon for massive neutropenia to lead to treatment being discontinued. The constipation, which may be severe, can be prevented with the prophylactic administration of laxatives .

Individual evidence

↑ This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.
↑ ^a ^b CHMP Assessment Report for Javlor , Committee on Medicinal Products for Human Use of the European Medicines Agency, October 2009.
↑ Assessment report - Variation , Committee on Medicinal Products for Human Use of the European Medicines Agency, December 2014.

[NV-1] This substance has either not yet been classified with regard to its hazardousness or a reliable and citable source has not yet been found.

[EPAR-2] CHMP Assessment Report for Javlor , Committee on Medicinal Products for Human Use of the European Medicines Agency, October 2009.

[3] Assessment report - Variation , Committee on Medicinal Products for Human Use of the European Medicines Agency, December 2014.