Duvelisib

Duvelisib
Systematic (IUPAC) name
8-Chloro-2-phenyl-3-[(1S)-1-(3H-purin-6-ylamino)ethyl]-1(2H)-isoquinolinone
Identifiers
CAS Number 1201438-56-3
ATC code None
PubChem CID 50905713
ChemSpider 28637766
KEGG D10555
Synonyms IPI-145
Chemical data
Formula C22H17ClN6O
Molar mass 416.86 g/mol

Duvelisib (INN,[1] previously known as IPI-145) is an inhibitor of PI3Kδ and PI3Kγ,[2] researched as a treatment for hematologic malignancies as well as a broad range of inflammatory conditions.[3]

Approvals and indications

As of April 2016 duvelisib has no approvals for marketing for clinical use.

Mechanism of action

By inhibiting the PI3K/AKT/mTOR pathway cancer cell growth/proliferation (dependant on this pathway) may be reduced.

Clinical trials

It has started two phase I clinical trials in hematologic cancers.[3] In July 2012 the phase I trial was expanded and two phase II trials were planned.[4][5]

Phase I results in patients with relapsed/refractory hematologic malignancies who had been previously treated with ibrutinib showed "clinical activity and a tolerable safety profile".[6]

A phase II trial for refractory indolent non-Hodgkin lymphoma is registered.[7]

A phase IIA study in asthma has reported preliminary results indicating improvement in lung function.[8] The ASPIRA trial, a Phase 2 study of duvelisib with methotrexate in patients with moderate-to-severe rheumatoid arthritis, was expected to report by end 2014.[8]

As of December 2015 there are four active phase III trials[9] including:

See also

References

  1. ↑ "International Nonproprietary Names for Pharmaceutical Substances (INN). Recommended International Nonproprietary Names: List 72" (PDF). World Health Organization. p. 393. Retrieved 16 April 2016.
  2. ↑ "Infinity Initiates Two Phase 1 Trials of IPI-145, a Potent Inhibitor of PI3K Delta and Gamma". finanznachrichten.de. 31 October 2011.
  3. 1 2 "Infinity commences two IPI-145 Phase 1 clinical trials for hematologic malignancies". Retrieved November 28, 2011.
  4. ↑ "Infinity Regains Worldwide Rights to PI3K, FAAH and Early Discovery Programs". 18 July 2012.
  5. ↑ Infinity Reports IPI-145 Phase 1 Data Showing Clinical Activity in B-Cell and T-Cell Malignancies at ASH Annual Meeting. Dec 2012
  6. ↑ Clinical Activity of Duvelisib (IPI-145), a Phosphoinositide-3-Kinase-δ,γ Inhibitor, in Patients Previously Treated with Ibrutinib. Dec 2014
  7. ↑ A Phase 2 Study of Duvelisib in Subjects With Refractory Indolent Non-Hodgkin Lymphoma (DYNAMO)
  8. 1 2 Infinity Reports Topline Data from Phase 2a Exploratory Study of Duvelisib in Patients with Mild, Allergic Asthma. Oct 2014
  9. ↑ Phase 3 trials
  10. ↑ Duvelisib With Obinutuzumab in Patients With CLL/SLL Previously Treated With a BTKi (SYNCHRONY)


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