What Kyprolis is used for and how to use it
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Kyprolis (carfilzomib) – Consumer Medicine Information

Manufacture: Amgen
Country: United States
Condition: Myeloma, Multiple (Multiple Myeloma)
Class: Antineoplastics, Proteasome inhibitors
Form: Liquid solution, Intravenous (IV)
Ingredients: carfilzomib

What is Kyprolis?

Kyprolis is a new drug being used to treat myeloma.

Like Velcade® (bortezomib), Kyprolis belongs to a group of drugs known as proteasome inhibitors. However, Kyprolis has been developed to specifically target a different area of the proteasome to Velcade. This is thought to make Kyprolis possibly more effective and potentially cause fewer side-effects than Velcade.

What are proteasomes?

Proteasomes are large molecules which are present in all cells in the body. They are involved in the removal, breakdown and recycling of damaged proteins or those that are no longer needed by the cell.

How does Kyprolis work?

Kyprolis works by permanently blocking the actions of proteasomes (Figure 1). As a consequence of blocking the actions of proteasomes, proteins build up and become toxic. This confuses the cell and causes it to die.

Multiplying myeloma cells rely more heavily on proteasomes than normal healthy cells, which divide slowly. They are therefore much more sensitive to Kyprolis.

Myeloma cells appear to be even more dependent on the actions of proteasomes than other types of cancer cells. This may be due to the need for the myeloma cell to dispose of the abnormal protein (paraprotein) it produces.

Through its actions of blocking the functioning of the proteasome, Kyprolis prevents the myeloma cells from growing and multiplying.


Figure 1. Kyprolis works by blocking the function of proteasomes

How is Kyprolis given?

Kyprolis is given as an intravenous infusion, lasting between 2 – 10 minutes. The recommended dosing of Kyprolis is 20 mg/m2 six times per 28-day cycle for the first cycle, and then 27 mg/m2 six times per 28-day cycle thereafter for all patients able to tolerate the higher dose.

Kyprolis can be given as a monotherapy (i.e. used on its own and not in combination with other drugs) but it has been shown to be most effective when used in combination with other anti-myeloma treatments such as Revlimid® (lenalidomide) and dexamethasone.

What evidence exists to support the use of Kyprolis?

Unlike Velcade which is commonly associated with peripheral neuropathy, Kyprolis has been demonstrated to cause very low rates of peripheral neuropathy (in less than 1% of patients). Peripheral neuropathy is a condition caused by damage to the nerves in the hands, feet, arms and legs.

Clinical trials to date have shown that Kyprolis produces effective and durable responses in relapsed patients, even in those refractory to two or more treatments.

Results from an ongoing large-scale Phase III clinical trial (called the ASPIRE trial) have shown the average progression free survival (the length of time before the myeloma starts to come back) for relapsed and/or refractory patients who received Kyprolis in combination with Revlimid and low-dose dexamethasone was 26.3 months, compared to 17.6 months for those who received Revlimid and dexamethasone only. Therefore, adding Kyprolis to Revlimid and dexamethasone increased the average length of remission or plateau by nearly nine months.

Kyprolis is also proving to be an effective initial treatment for newly diagnosed myeloma patients.

A Phase III clinical trial has shown that Kyprolis when used as a monotherapy (i.e. used on its own and not in combination with other drugs) does not help patients to live longer.

What are the known possible side-effects of Kyprolis?

The most common side-effects of Kyprolis that have been reported include: fatigue, low platelet levels (thrombocytopenia); low red blood cell levels (anaemia); nausea, difficulty breathing, diarrhoea and fever.

Kyprolis can also cause heart problems or worsen pre-existing heart conditions. Patients being treated with Kyprolis will therefore be monitored carefully during treatment.