Buparlisib, a PI3K inhibitor, demonstrates acceptable tolerability and preliminary activity in a phase I trial of patients with advanced leukemias
Sign Up to like & getrecommendations! Published in 2017 at "American Journal of Hematology"
DOI: 10.1002/ajh.24568
Abstract: Phosphatidylinositol‐3‐kinase (PI3K) signaling plays a crucial role in oncogene‐mediated tumor growth and proliferation. Buparlisib (BKM120) is an oral pan‐class I PI3K inhibitor. This phase I study was conducted to determine the dose limiting toxicity (DLT)… read more here.
Keywords: phase; pi3k; buparlisib; day ... See more keywords
COASTAL: A PHASE 3 STUDY OF THE PI3Kδ INHIBITOR ZANDELISIB WITH RITUXIMAB (R) VERSUS IMMUNOCHEMOTHERAPY IN PATIENTS WITH RELAPSED INDOLENT NON‐HODGKIN’S LYMPHOMA (INHL)
Sign Up to like & getrecommendations! Published in 2021 at "Hematological Oncology"
DOI: 10.1002/hon.174_2880
Abstract: TPS7573Background: Patients (pts) with iNHL treated with front-line immunochemotherapy may benefit from an alternative, chemotherapy-free regimen at relapse. Zandelisib, a potent, selective, and st... read more here.
Keywords: immunochemotherapy; study pi3k; coastal phase; inhibitor zandelisib ... See more keywords
LY294002, a PI3K inhibitor, attenuates Tourette syndrome in rats
Sign Up to like & getrecommendations! Published in 2017 at "Metabolic Brain Disease"
DOI: 10.1007/s11011-017-0051-z
Abstract: The present study was designed to investigate the effects of LY294002 on Tourette syndrome (TS) in rats. TS model was induced in rats by DOI (the selective 5-HT2A/2C agonist 1- (2, 5- dimethoxy −4 -… read more here.
Keywords: syndrome rats; pi3k akt; ly294002 pi3k; pi3k inhibitor ... See more keywords
Calcium signaling mediated by aminergic GPCRs is impaired by the PI3K inhibitor LY294002 and its analog LY303511 in a PI3K-independent manner.
Sign Up to like & getrecommendations! Published in 2020 at "European journal of pharmacology"
DOI: 10.1016/j.ejphar.2020.173182
Abstract: The phosphoinositide 3-kinase (PI3K) inhibitor LY294002 (LY294) and its much less active analog LY303511 (LY303) constitute the paired probe that is commonly used to demonstrate the involvement of PI3K in intracellular signaling. We studied effects… read more here.
Keywords: pi3k inhibitor; inhibitor ly294002; analog ly303511; aminergic gpcrs ... See more keywords
The Class I PI3K inhibitor S14161 induces autophagy in malignant blood cells by modulating the Beclin 1/Vps34 complex.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of pharmacological sciences"
DOI: 10.1016/j.jphs.2017.07.001
Abstract: S14161 is a pan-Class I PI3K inhibitor that induces blood cancer cell death, but its mechanism is largely unknown. In the present study, we evaluated the role of S14161 in autophagy, an emerging event in… read more here.
Keywords: s14161; pi3k inhibitor; beclin; class pi3k ... See more keywords
Discovery of a Potent and Selective PI3Kδ Inhibitor (S)-2,4-Diamino-6-((1-(7-fluoro-1-(4-fluorophenyl)-4-oxo-3-phenyl-4H-quinolizin-2-yl)ethyl)amino)pyrimidine-5-carbonitrile with Improved Pharmacokinetic Profile and Superior Efficacy in Hematological Cancer Models.
Sign Up to like & getrecommendations! Published in 2020 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.0c01264
Abstract: PI3Kδ inhibitors have been approved for B-cell malignancies like CLL, small lymphocytic lymphoma, and so forth. However, currently available PI3Kδ inhibitors are nonoptimal, showing weakness against at least one of the several important properties: potency,… read more here.
Keywords: pharmacokinetic profile; pi3k inhibitor; profile; efficacy ... See more keywords
Discovery of AZD8154, a Dual PI3Kγδ Inhibitor for the Treatment of Asthma.
Sign Up to like & getrecommendations! Published in 2021 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.1c00434
Abstract: Starting from our previously described PI3Kγ inhibitors, we describe the exploration of structure-activity relationships that led to the discovery of highly potent dual PI3Kγδ inhibitors. We explored changes in two positions of the molecules, including… read more here.
Keywords: discovery azd8154; azd8154 dual; discovery; dual pi3k ... See more keywords
Polymyalgia rheumatica development in a patient under PI3K inhibitor therapy for chronic lymphocytic leukaemia
Sign Up to like & getrecommendations! Published in 2017 at "BMJ Case Reports"
DOI: 10.1136/bcr-2017-221065
Abstract: We report a patient with chronic lymphocytic leukaemia (CLL) who was treated with idelalisib, a PI3Kδ inhibitor with rituximab. After 20 weeks of treatment, the patient developed classical signs and symptoms of polymyalgia rheumatica (PMR)… read more here.
Keywords: lymphocytic leukaemia; pi3k inhibitor; chronic lymphocytic; patient ... See more keywords
Peptidic microarchitecture-trapped tumor vaccine combined with immune checkpoint inhibitor or PI3Kγ inhibitor can enhance immunogenicity and eradicate tumors
Sign Up to like & getrecommendations! Published in 2022 at "Journal for Immunotherapy of Cancer"
DOI: 10.1136/jitc-2021-003564
Abstract: Background With the rapid development of immune checkpoint inhibitors and neoantigen (NeoV)-based personalized tumor vaccines, tumor immunotherapy has shown promising therapeutic results. However, the limited efficacy of available tumor vaccines impedes the development of personalized… read more here.
Keywords: tumor; pma neov; tumor vaccine; pi3k inhibitor ... See more keywords
On-Target Pharmacodynamic Activity of the PI3K Inhibitor Copanlisib in Paired Biopsies from Patients with Malignant Lymphoma and Advanced Solid Tumors
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DOI: 10.1158/1535-7163.mct-19-0466
Abstract: The PI3K inhibitor copanlisib has efficacy and manageable safety in patients with indolent lymphoma and solid tumors. Pharmacodynamic effects relative to copanlisib dose and plasma exposure were evaluated. Patients with lymphoma or solid tumors received… read more here.
Keywords: copanlisib; pi3k inhibitor; inhibitor copanlisib; solid tumors ... See more keywords
Novel Miniaturized Drug Conjugate Leverages HSP90-driven Tumor Accumulation to Overcome PI3K Inhibitor Delivery Challenges to Solid Tumors
Sign Up to like & getrecommendations! Published in 2020 at "Molecular Cancer Therapeutics"
DOI: 10.1158/1535-7163.mct-19-0964
Abstract: The PI3K pathway is considered a master regulator for cancer due to its frequent activation, making it an attractive target for pharmacologic intervention. While substantial efforts have been made to develop drugs targeting PI3K signaling,… read more here.
Keywords: drug; pi3k inhibitor; tumor; delivery ... See more keywords