PX-866

inhibitor of phosphoinositide-3-kinase signaling with antitumor activity; structure in first source

Also Known As:

acetic acid (1S,4E,10R,11R,13S,14R)-(4-diallylaminomethylene-6-hydroxy-1-methoxymethyl-10,13-dimethyl-3,7,17-trioxo-1,3,4,7,10,11,12,13,14,15,16,17-dodecahydro-2-oxa-cyclopenta(a)phenanthren-11-yl)ester

Networked: 28 relevant articles (1 outcomes, 12 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Polycyclic Compounds: 6
- Fused-Ring Compounds
  - Steroids: 70059
    - Gonanes: 2
      - PX-866: 28

Experts

1.	Powis, Garth: 8 articles (04/2011 - 07/2004)
2.	Bowles, Daniel W: 6 articles (12/2016 - 08/2012)
3.	Walker, Luke: 5 articles (01/2018 - 07/2014)
4.	Jimeno, Antonio: 5 articles (12/2016 - 08/2012)
5.	Hausman, Diana: 4 articles (12/2016 - 07/2014)
6.	Ihle, Nathan T: 4 articles (01/2009 - 07/2004)
7.	Wipf, Peter: 4 articles (01/2009 - 07/2004)
8.	Schnadig, Ian: 3 articles (12/2016 - 07/2014)
9.	Spira, Alexander: 3 articles (12/2016 - 07/2014)
10.	Peek, Gregory W: 3 articles (01/2016 - 01/2016)

Related Diseases

1.	Squamous Cell Carcinoma of Head and Neck 08/01/2013 - "The PI3K inhibitor PX-866 had anti-tumor efficacy in HNSCC models with PIK3CA alterations. " 01/01/2019 - "PI3K inhibitors such as PI-103, PI-828 and PX-866 may be developed as potential therapeutic agents for effective treatment of oral squamous cell carcinoma (OSCC) patients, associated with activated PI3K/Akt pathway." 04/01/2015 - "This randomized phase 2 study evaluated PX-866 combined with docetaxel in patients with advanced, refractory HNSCC. " 03/01/2015 - "This randomized phase II study evaluated PX-866 combined with cetuximab in patients with advanced, refractory HNSCC. " 04/01/2015 - "The addition of PX-866 to docetaxel did not improve PFS, RR, or OS in patients with advanced, refractory HNSCC without molecular pre-selection."
2.	Neoplasms (Cancer) 08/01/2012 - "The objectives of the study were to evaluate the maximum tolerated dose (MTD), safety, pharmacodynamics, pharmacokinetics, and antitumor activity of PX-866 in patients with incurable cancers. " 04/01/2011 - "Our findings suggest that inhibition of these pathways might increase tumor sensitivity to PX-866 and therefore represent a potential clinical therapeutic strategy." 06/01/2010 - "In vivo, PX-866 inhibited subcutaneous tumor growth and increased the median survival time of animals with intracranial tumors. " 01/01/2009 - "The level of activation of PI3K signaling measured by tumor phosphorylated Ser(473)-Akt was insufficient to predict in vivo antitumor response to PX-866. " 01/01/2009 - "Mutant PI3K (PIK3CA) and loss of PTEN activity were sufficient, but not necessary, as predictors of sensitivity to the antitumor activity of the PI3K inhibitor PX-866 in the presence of wild-type Ras, whereas mutant oncogenic Ras was a dominant determinant of resistance, even in tumors with coexisting mutations in PIK3CA. "
3.	Glioblastoma (Glioblastoma Multiforme) 09/01/2015 - "Phase II study of PX-866 in recurrent glioblastoma." 04/01/2011 - "In this study, we performed a synthetic lethality screen to identify genes or pathways whose inactivation, in combination with the PI3K inhibitors PX-866 and NVPBEZ-235, might result in a lethal phenotype in glioblastoma multiforme (GBM) cells. " 06/01/2010 - "PX-866 inhibited the invasive and angiogenic capabilities of cultured glioblastoma cells. " 06/01/2010 - "We report that a new irreversible PI3K inhibitor, PX-866, shows potent inhibitory effects on the PI3K/Akt signaling pathway in glioblastoma. " 06/01/2010 - "Cellular and in vivo activity of a novel PI3K inhibitor, PX-866, against human glioblastoma."
4.	Non-Small-Cell Lung Carcinoma (Carcinoma, Non-Small Cell Lung) 01/01/2009 - "Our studies have shown that pioglitazone does not inhibit the antitumor activity of PX-866 in A-549 non-small cell lung cancer and HT-29 colon cancer xenografts. " 07/01/2014 - "A randomized, phase 2 trial of Docetaxel with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic non-small-cell lung cancer." 09/01/2005 - "The phosphatidylinositol-3-kinase inhibitor PX-866 overcomes resistance to the epidermal growth factor receptor inhibitor gefitinib in A-549 human non-small cell lung cancer xenografts."
5.	Squamous Cell Neoplasms (Squamous Cell Cancer) 04/01/2015 - "A randomized, phase 2 trial of docetaxel with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic head and neck squamous cell cancer." 03/01/2015 - "A randomized, phase II trial of cetuximab with or without PX-866, an irreversible oral phosphatidylinositol 3-kinase inhibitor, in patients with relapsed or metastatic head and neck squamous cell cancer."

Related Drugs and Biologics

1.	PI103
2.	Phosphatidylinositol 3-Kinase (1 Phosphatidylinositol 3 Kinase)
3.	Cetuximab (Erbitux)
4.	Docetaxel (Taxotere)
5.	Vemurafenib
6.	Pioglitazone (Actos)
7.	3-methyladenine
8.	Raloxifene Hydrochloride (Evista)
9.	Cyclin D1
10.	Estrogen Receptors

Related Therapies and Procedures

1.	Castration
2.	Withholding Treatment
3.	Therapeutics