Duvelisib: First Global Approval

Blair, Hannah A.

doi:10.1007/s40265-018-1013-4

Cited by 92 publications

(57 citation statements)

References 12 publications

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“…Consequently, following with the world's first selective PI3Kδ inhibitor CAL-101 was approved by the FDA for the treatment of FL, CLL and SLL in 2014 [315] [NCT01282424, NCT02136511], the PI3K/AKT inhibitors have shown remarkable activity in an increasing subset of patients with NHL [316] (Tables 2, 3). Copanlisib (BAY 80-6946) and Duvelisib (IPI-145) are newly approved PI3K inhibitors that offer objective, although relatively short-lasting, responses in patients with heavily pre-treated FL and other NHL, and more such targeted agents may be approved soon [307,[317][318][319][320] (Tables 2 and 3).…”

Section: Description Of the Pi3k/akt Pathway In The Hemato-immune Sysmentioning

confidence: 99%

Role of PI3K/AKT pathway in cancer: the framework of malignant behavior

et al. 2020

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Given that the PI3K/AKT pathway has manifested its compelling influence on multiple cellular process, we further review the roles of hyperactivation of PI3K/AKT pathway in various human cancers. We state the abnormalities of PI3K/AKT pathway in different cancers, which are closely related with tumorigenesis, proliferation, growth, apoptosis, invasion, metastasis, epithelial-mesenchymal transition, stem-like phenotype, immune microenvironment and drug resistance of cancer cells. In addition, we investigated the current clinical trials of inhibitors against PI3K/AKT pathway in cancers and found that the clinical efficacy of these inhibitors as monotherapy has so far been limited despite of the promising preclinical activity, which means combinations of targeted therapy may achieve better efficacies in cancers. In short, we hope to feature PI3K/ AKT pathway in cancers to the clinic and bring the new promising to patients for targeted therapies.

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Section: Description Of the Pi3k/akt Pathway In The Hemato-immune Sysmentioning

confidence: 99%

Role of PI3K/AKT pathway in cancer: the framework of malignant behavior

et al. 2020

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“…[72][73][74] In September 2018, duvelisib was approved by the FDA for treatment of patients with CLL who have had at least 2 prior therapies. 75 Umbralisib (TGR-12032) also has been shown to have clinical activity, particularly in combination with ibrutinib. 76 However, combination of idelalisib with other kinase inhibitors (e.g., Syk) has resulted in unacceptable toxicity.…”

Section: Kinasementioning

confidence: 99%

Targeted Therapy in Chronic Lymphocytic Leukemia

Kipps

Choi

2019

Cancer J

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Despite a prevailing view that advances in cancer therapy will come through selective targeting of enzymes encoded by mutated oncogenes responsible for the neoplastic phenotype, recent advances in the treatment of patients with chronic lymphocytic leukemia (cLL) have instead exploited knowledge of its biology. indeed, cLL cells depend on interactions with cells and soluble factors present in the tumor microenvironment for proliferation and survival. B-cell receptor signaling and chemokine-receptor signaling play prominent roles. Elucidation of these signaling pathways has defined physiologic targets for drugs, such as ibrutinib, which inhibit Bruton tyrosine kinase and are therapeutically effective. The characteristic high-level expression of BCL2 in CLL that can enhance leukemia-cell survival has now become an Achilles heel targeted by clinically effective drugs such as venetoclax. Here we discuss advances in such targeted therapy and highlight other disease attributes, such as the distinctive expression of ROR1, which may be targeted for clinical benefit, alone or in combination with other targeted therapies.

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“…Up to date several PI3K isoform-specific inhibitors were developed and are in the market toward blood cancers. The first in class inhibitors registered for hematologic cancer therapy are idelalisib (specific for PI3Kδ), duvelisib (specific for PI3Kδ and γ) and copanlisib (specific for PI3Kα and δ) [6][7][8]. However, the data indicating toxicity of the above-mentioned drugs exclude their usage in patients not suffering from a life-threating disease.…”

Section: Introductionmentioning

confidence: 99%

Preclinical characterization of CPL302-253, a selective inhibitor of PI3Kδ, as the candidate for the inhalatory treatment and prevention of Asthma

et al. 2020

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Asthma is a common chronic inflammatory disease. Although effective asthma therapies are available, part of asthmatic population do not respond to these treatment options. In this work we present the result of development of CPL302-253 molecule, a selective PI3Kδ inhibitor. This molecule is intended to be a preclinical candidate for dry powder inhalation in asthma treatment. Studies we performed showed that this molecule is safe and effective PI3Kδ inhibitor that can impact many immune functions. We developed a short, 15-day HDM induced asthma mouse model, in which we showed that CPL302-253 is able to block inflammatory processes leading to asthma development in vivo.

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Duvelisib: First Global Approval

Cited by 92 publications

References 12 publications

Role of PI3K/AKT pathway in cancer: the framework of malignant behavior

Role of PI3K/AKT pathway in cancer: the framework of malignant behavior

Targeted Therapy in Chronic Lymphocytic Leukemia

Preclinical characterization of CPL302-253, a selective inhibitor of PI3Kδ, as the candidate for the inhalatory treatment and prevention of Asthma

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