spec sheet8 rows
Alisertib An orally available, ATP-competitive small-molecule inhibitor of Aurora A kinase, an enzyme that regulates cell division. Developed by Takeda and later licensed to Puma Biotechnology, it was investigated across multiple cancer types including peripheral T-cell lymphoma, neuroendocrine prostate cancer, and acute myeloid leukemia.
- Showed single-agent and combination activity across several cancer types in clinical trials, including leukemia, lymphoma, and ovarian cancer
- Selectively targets Aurora A over the closely related Aurora B kinase, aiming for a more precise mechanism than older antimitotic drugs
- Common trial side effects included neutropenia (low white blood cell counts), fatigue, hair loss, and gastrointestinal upset
Overview
A serious oncology drug candidate with real clinical trial data behind it; its lead lymphoma trial got terminated in 2015 but research in other cancers continued.
Mechanism
Alisertib selectively and reversibly inhibits Aurora A kinase, a mitotic enzyme that regulates centrosome maturation and mitotic spindle assembly, at more than 200-fold greater potency than the closely related Aurora B kinase. This disrupts spindle assembly and chromosome segregation, blocking cell division. In neuroendocrine prostate cancer, it also disrupts the interaction between Aurora A and the oncoprotein N-myc, suppressing N-myc-driven tumor growth.
receptor fingerprint
Aurora A kinaseInhibitor
Dosingtypical ranges, not medical advice
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Safetyrisks and cautions, not medical advice
In clinical trials, alisertib was generally tolerable but commonly caused myelosuppression (low blood cell counts, particularly neutropenia), fatigue, alopecia (hair loss), and gastrointestinal side effects typical of antimitotic chemotherapy agents. Its pivotal phase 3 trial in peripheral T-cell lymphoma was terminated in 2015.
Subjective profileweighing the evidence above
A cancer drug that belongs to an oncologist running a protocol, not to a reader. The Aurora A selectivity is genuinely elegant pharmacology, but the pivotal phase 3 in T-cell lymphoma was terminated in 2015 and the side effects are standard antimitotic chemotherapy: neutropenia, fatigue and hair loss.
Resources
This entry is here for reference.
Research
- 1.An exploratory phase 2 study of investigational Aurora A kinase inhibitor alisertib (MLN8237) in acute myelogenous leukemia and myelodysplastic syndromes
- 2.Phase II study of MLN8237 (alisertib), an investigational Aurora A kinase inhibitor, in patients with platinum-resistant or -refractory epithelial ovarian, fallopian tube, or primary peritoneal carcinoma
2 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
What is Alisertib used for?
It has been investigated as an experimental cancer treatment across several tumor types, including lymphoma, leukemia, ovarian cancer, and neuroendocrine prostate cancer, though it remains investigational rather than approved.
How does Alisertib work?
It selectively inhibits Aurora A kinase, an enzyme cancer cells need to properly assemble their mitotic spindle and divide, causing division errors that halt tumor growth.
Is Alisertib well-researched?
Yes, relative to most compounds in this reference; it has been through numerous phase 1 and phase 2 clinical trials and one terminated phase 3 trial, though it has not achieved regulatory approval.
Adverse effects
- Common trial side effects included neutropenia (low white blood cell counts), fatigue, hair loss, and gastrointestinal upset
Notes and cautions
- Its lead phase 3 trial in peripheral T-cell lymphoma was terminated in 2015