PKI 166

Also Known As:

4-(4-((1-phenylethyl)amino)-7H-pyrrolo(2,3-d)pyrimidin-6-yl)-phenol, R-; 4-phenethylamino-6-(yderoxyl)phenyl-7H-pyrrolo(2,3-d)pyrimidine; CGP 75166; CGP-75166; CGP75166; PKI-166; PKI166

Networked: 34 relevant articles (4 outcomes, 4 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Pyrroles: 369
      - PKI 166: 34
  - Pyrimidines: 510
    - PKI 166: 34

Experts

1.	Fidler, Isaiah J: 13 articles (05/2008 - 04/2002)
2.	Baker, Cheryl H: 4 articles (06/2006 - 04/2002)
3.	Bucana, Corazon D: 3 articles (01/2004 - 09/2002)
4.	Killion, Jerald J: 3 articles (03/2003 - 08/2002)
5.	Fabbro, Doriano: 2 articles (06/2008 - 02/2002)
6.	Kim, Sun-Jin: 2 articles (05/2008 - 03/2003)
7.	Hynes, Nancy E: 2 articles (06/2005 - 11/2004)
8.	O'Reilly, Terence: 2 articles (06/2005 - 02/2002)
9.	Mellinghoff, Ingo K: 2 articles (01/2005 - 09/2002)
10.	Sawyers, Charles L: 2 articles (01/2005 - 09/2002)

Related Diseases

1.	Neoplasms (Cancer) 01/01/2005 - "Treatment with PKI-166 markedly lowered tumor (18)F-FLT uptake within 48 h of drug exposure; within 1 wk (18)F-FLT uptake decreased by 79%. " 12/01/2004 - "In addition, PKI166 enhanced markedly the chemosensitivities of metastatic cancer cell sublines to various anticancer drugs in comparison with those of low metastatic cancer cells. " 08/01/2003 - "After lingual tumors developed, mice were randomized into four groups (n = 10): (a) oral PKI166 (100 mg/kg); (b) i.p. " 08/01/2002 - "PKI166 significantly reduced tumor growth in mice treated for 1 month with oral PKI166 in a dose-dependent fashion. " 08/01/2002 - "Next, daily doses of PKI166 (0, 10, or 50 mg/kg) were delivered by orogastric lavage for 28 days and the animals were observed for tumor growth. "
2.	Prostatic Neoplasms (Prostate Cancer) 09/15/2002 - "To investigate the relationship between ErbB-RTK signaling and androgen in genetically unmanipulated human prostate cancer, we performed biochemical and biological studies with the dual ErbB1/ErbB2 RTK inhibitor PKI-166 using human prostate cancer xenograft models with isogenic sublines reflecting the transition from androgen-dependent to androgen-independent growth. " 09/15/2002 - "Growth inhibitory effects of the dual ErbB1/ErbB2 tyrosine kinase inhibitor PKI-166 on human prostate cancer xenografts." 03/01/2003 - "We determined whether blockade of the epidermal growth factor receptor (EGF-R) signaling pathway by oral administration of the EGF-R tyrosine kinase inhibitor (PKI 166) alone or in combination with injectable Taxol inhibits the growth of PC-3MM2 human prostate cancer cells in the bone of nude mice. "
3.	Ovarian Neoplasms (Ovarian Cancer) 09/01/2008 - "We reviewed data identified by searches of MEDLINE, PubMed, and abstracts from the proceedings of the American Society of Clinical Oncology meetings from 1998 to 2006, with the search terms "Ovarian Cancer,""EGFR,""gefitinib, ZD1839, Iressa,""erlotinib, OSI-774, Tarceva,""CI-1033,"" GW 572016, lapatinib,""PKI-166,""EKB 569,""anti-EGFR antibodies,""trastuzumab, Herceptin,""cetuximab, Erbitux, IMC-C225,""matuzumab, EMD 72000,""panitumamab, ABX-EGF,""pertuzumab," and "vandetanib, rINN, Zactima, ZD6474." Phase II trials of both small molecule inhibitors of EGFR- and antibody-based inhibitors are currently ongoing in ovarian cancer and emerging data suggest that their activity in unselected women with advanced or recurrent ovarian cancer is modest, when utilized as a single agent. "
4.	Neoplasm Metastasis (Metastasis) 01/01/2012 - "PKI 166 is used to determine the effects of redox sensitive inhibition of EGFR, metastasis and apoptosis in epidermoid carcinoma. " 11/01/2002 - "Treatment with PKI166 and, more so, PKI166 plus gemcitabine significantly inhibited lung metastasis, corresponding to a significant increase in overall length of survival. " 08/01/2001 - "Daily oral PKI 166 or thrice weekly oral PKI 166 in combination with injected gemcitabine produced 97% and 95% decreases in volume of pancreatic cancers and significant inhibition of lymph node and liver metastasis. " 06/01/2000 - "We determined whether down-regulation of the epidermal growth factor-receptor (EGF-R) signaling pathway by oral administration of a novel EGF-R tyrosine kinase inhibitor (PKI166) alone or in combination with gemcitabine (administered i.p.) can inhibit growth and metastasis of human pancreatic carcinoma cells implanted into the pancreas of nude mice. " 04/01/2002 - "We determined whether concurrent blockage of vascular endothelial growth factor (VEGF) receptor and epidermal growth factor (EGF) receptor signaling by two novel tyrosine kinase inhibitors, PTK 787 and PKI 166, respectively, can inhibit angiogenesis and, hence, the growth and metastasis of human pancreatic carcinoma in nude mice. "
5.	Pancreatic Neoplasms (Pancreatic Cancer) 08/01/2001 - "Daily oral PKI 166 or thrice weekly oral PKI 166 in combination with injected gemcitabine produced 97% and 95% decreases in volume of pancreatic cancers and significant inhibition of lymph node and liver metastasis. " 06/01/2000 - "Therapy beginning 7 days after orthotopic injection of L3.6pl human pancreatic cancer cells reduced the volume of pancreatic tumors by 59% in mice treated with gemcitabine only, by 45% in those treated with PKI166 only, and by 85% in those given both drugs. " 04/01/2004 - "Because PKI 166 prevented the activation of PI3K/Akt/NF-kappa B and MAPK(Erk) pathways, the combination of this tyrosine kinase inhibitor with gemcitabine should be an effective therapy for pancreatic cancer." 06/01/2000 - "We determined whether down-regulation of the epidermal growth factor-receptor (EGF-R) signaling pathway by oral administration of a novel EGF-R tyrosine kinase inhibitor (PKI166) alone or in combination with gemcitabine (administered i.p.) can inhibit growth and metastasis of human pancreatic carcinoma cells implanted into the pancreas of nude mice. " 08/01/2001 - "We determined the optimal administration schedule of a novel epidermal growth factor receptor (EGFR) protein tyrosine kinase inhibitor (PKI), PKI 166 (4-(R)-phenethylamino-6-(hydroxyl)phenyl-7H-pyrrolo[2.3-d]-pyrimidine), alone or in combination with gemcitabine (administered i.p.) for therapy of L3.6pl human pancreatic carcinoma growing in the pancreas of nude mice. "

Related Drugs and Biologics

1.	Epidermal Growth Factor (EGF)
2.	Paclitaxel (Taxol)
3.	Vascular Endothelial Growth Factor A (Vascular Endothelial Growth Factor)
4.	Interleukin-8 (Interleukin 8)
5.	ErbB Receptors (EGF Receptor)
6.	Phosphotransferases (Kinase)
7.	Proliferating Cell Nuclear Antigen (PCNA)
8.	Tyrosine Kinase Inhibitors
9.	Gefitinib (Iressa)
10.	Erlotinib Hydrochloride (CP 358,774)

Related Therapies and Procedures

1.	Therapeutics
2.	Oral Administration
3.	Drug Therapy (Chemotherapy)
4.	Injections