On this page we will be discussing P13 kinase inhibitors and the main types that are currently being used in the treatment of some lymphomas.
What are P13 kinase inhibitors?
Cells receive signals that keep them alive and make them divide. These signals are sent along different signalling pathways inside the body. Blocking either the signal or a key part of the pathway can make cells die or stop the lymphoma from growing. Certain signalling pathways are more important in some types of lymphoma than in others.
Scientists do not yet fully understand how all the various pathways are linked. There are different cell signal blockers that are used in the treatment of lymphoma that include BTK inhibitors and PI3K inhibitors.
P13 kinase inhibitors work by inhibiting PI3K (phosphatidylinositol 3-kinase) which is an enzyme that is overactive in B-cell cancers. By blocking the effects of this enzyme, it affects the growth of malignant lymphocyte cells and causing cell death. Types of PI3 kinase inhibitors that are currently being used in the treatment of lymphoma.
- Idelalisib
- Umbralisib
Idelalisib (Zydelig)
Idelalisib is an oral anti-neoplastic medicine that targets B-cell cancers.
Idelalisib works by inhibiting PI3K (phosphatidylinositol 3-kinase) which is an enzyme that is overactive in B-cell cancers. By blocking the effects of this enzyme, it affects the growth of malignant lymphocyte cells and causing cell death.
Indications of use in lymphoma
The current use of Idelalisib in lymphoma and CLL include:
- CD20 positive B-cell chronic lymphocytic leukaemia (CLL) / small lymphocytic lymphoma (SLL) in patients who have relapsed, and chemo-immunotherapy is not considered suitable. For patients with relapsed CLL or SLL. First line treatment with a 17p deletion or TP53 mutation. Given in combination with rituximab for which chemo-immunotherapy is not considered suitable.
- Follicular lymphoma, as monotherapy where disease is refractory to at least 2 prior systemic therapies including both rituximab and an alkylating agent. Given as a monotherapy for the treatment of refractory FL For patients that are refractory to at least two prior systemic therapies. Patients must be refractory to both rituximab and an alkylating agent.
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There are several clinical trials currently available in Australia and internationally investigating Idelalisib as a single therapy and in combination with other therapies. To find out more about clinical trials and how you can find one for you, see the ‘clinical trials’ page and/or speak to your doctor.
How is it given?
- Administer orally TWICE a day
- To be swallowed whole with a glass of water; do not break, crush or chew
- May be taken with or without food
- If a dose is missed and it is less than 6 hours late, it should be taken as soon as the patient remembers. If it is more than 6 hours late, the patient should not take the missed dose.
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You take Idelalisib every day until your lymphoma stops responding to it, unless side effects are bad enough to make you stop treatment. You might be treated with Idelalisib for years.
Possible side effects
- Diarrhoea or colitis
- Hepatotoxicity
- Rash
- Pneumonitis
- Serious infection (e.g. CMV or PJP)
- Fever or severe chills
Umbralisib
Umbralisib is a type of targeted drug called a ‘cell signal blocker’. It blocks signals that B cells send to help them stay alive and divide. It works in a similar way to Idelalisib, which is a cell signal blocker that is already used for some types of non-Hodgkin lymphoma (NHL).
Umbralisib is a dual inhibitor of PI3K-delta and CK1-epsilon.
Indications
In development as a treatment for patients with:
- Previously treated marginal zone lymphoma (MZL)
- Follicular lymphoma (FL)
Administration
- Tablet
- Given once daily
- Given every day for as long as the treatment is helping you
Possible side-effects
- Diarrhoea
- Nausea
- Fatigue
- Neutropenia
- Anaemia
- Thrombocytopenia
