Myeloid Leukemia

Imetelstat

Telomerase Inhibitor

Table of contents

What is imetelstat used for?

Imetelstat blocks the enzyme telomerase.


It treats myelodysplastic syndromes and acute myeloid leukemia.

What is the mechanism of action of imetelstat?

Cells use telomerase to maintain telomeres on the ends of chromosomes.

The activity of telomerase is a lot higher in cancer cells.

Imetelstat attaches to and stops telomerase, which stops cancer cells from growing.

What are the contraindications of imetelstat?

The liver and kidney play a major role in processing imetelstat in the body

However, where the kidney and liver are not functioning properly, it can cause the drug to build up leading to more side effects. 

That is why people with severe liver or kidney problems should not take imetelstat.

Important imetelstat prescribing safety information.

High exposure to imetelstat can lead to low levels of platelets in the blood.

Low platelet levels can then lead to bruising and bleeding.

So it's important to monitor platelet count while on imetelstat to adjust and get the dose just right.

Additionally, regularly check for anti-drug antibodies to detect possible changes in how effective imetelstat is.

Imetelstat patient counselling advice.

Inform patients about possible imetelstat side effects which include: low platelets, tiredness, nausea, and diarrhoea.

Advise patients to report unusual bleeding or bruising, which could indicate low platelet levels.

Encourage good self-care and seek immediate help for severe symptoms or signs of infection.

References

1. Bruedigam, C., Porter, A.H., Song, A., Vroeg in de Wei, G., Stoll, T., Straube, J., Cooper, L., Cheng, G., Kahl, V.F.S., Sobinoff, A.P., Ling, V.Y., Jebaraj, B.M.C., Janardhanan, Y., Haldar, R., Bray, L.J., Bullinger, L., Heidel, F.H., Kennedy, G.A., Hill, M.M. and Pickett, H.A. (2023). Imetelstat-mediated alterations in fatty acid metabolism to induce ferroptosis as a therapeutic strategy for acute myeloid leukemia. Nature Cancer, [online] pp.1–19. doi:https://doi.org/10.1038/s43018-023-00653-5. Link


2. González‐Sales, M., Lennox, A.L., Huang, F., Pamulapati, C., Wan, Y., Sun, L., Berry, T., Kelly Behrs, M., Feller, F. and Morcos, P.N. (2024). Population pharmacokinetics of imetelstat, a first‐in‐class oligonucleotide telomerase inhibitor. CPT Pharmacometrics & Systems Pharmacology, 13(7), pp.1264–1277. doi:https://doi.org/10.1002/psp4.13160. Link


3. Uwe Platzbecker, Santini, V., Fenaux, P., Sekeres, M.A., Savona, M.R., Madanat, Y.F., María Díez-Campelo, Valcárcel, D., Illmer, T., Jonášová, A., Bělohlávková, P., Sherman, L., Berry, T., Dougherty, S., Shah, S., Xia, Q., Sun, L., Wan, Y., Huang, F. and Annat Ikin (2023). Imetelstat in patients with lower-risk myelodysplastic syndromes who have relapsed or are refractory to erythropoiesis-stimulating agents (IMerge): a multinational, randomised, double-blind, placebo-controlled, phase 3 trial. The Lancet. doi:https://doi.org/10.1016/s0140-6736(23)01724-5. Link

 

4. Ziedan, M., Salah, D. and Ayman, M. (2023). Therapeutic Impact of Telomerase Inhibitor Imetelstat: a Literature Review. International Journal of Advanced Health Science and Technology, 3(2). doi:https://doi.org/10.35882/ijahst.v3i2.238. Link