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KW-2450

an inhibitor of aurora A and B kinases with antineoplastic activity; structure in first source

Networked: 3 relevant articles (0 outcomes, 1 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Pyrazoles: 61
      - Indazoles: 179
        KW-2450: 3
  - Piperazines: 26
    - KW-2450: 3
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Indazoles: 179
      - KW-2450: 3

Experts

1.	Akinaga, Shiro: 2 articles (01/2018 - 04/2016)
2.	Maekawa, Yoshimi: 2 articles (01/2018 - 04/2016)
3.	Nakashima, Daisuke: 2 articles (01/2018 - 04/2016)
4.	Ueno, Naoto T: 2 articles (01/2018 - 12/2015)
5.	Fouad, Tamer M: 1 article (01/2018)
6.	Kaito, Hidekuni: 1 article (01/2018)
7.	Koizumi, Fumito: 1 article (01/2018)
8.	Ota, Toshio: 1 article (01/2018)
9.	Shimizu, Makiko: 1 article (01/2018)
10.	Shiraishi, Norihiko: 1 article (01/2018)

Related Diseases

1.	Hyperglycemia 04/01/2016 - "The maximum tolerated dose of KW-2450 was 37.5 mg once daily continuously; dose-limiting toxicity occurred in two of six patients at 50 mg/day (both grade 3 hyperglycemia) and in one of seven patients at 37.5 mg/day (grade 3 rash). " 01/01/2018 - "In the phase I study, dose-limiting toxicity (DLT; grade 3 rash and grade 3 hyperglycemia, respectively) occurred in two of three patients at the dose of KW-2450 25 mg/day plus lapatinib 1500 mg/day and letrozole 2.5 mg/day. "
2.	Exanthema (Rash) 04/01/2016 - "The maximum tolerated dose of KW-2450 was 37.5 mg once daily continuously; dose-limiting toxicity occurred in two of six patients at 50 mg/day (both grade 3 hyperglycemia) and in one of seven patients at 37.5 mg/day (grade 3 rash). " 01/01/2018 - "In the phase I study, dose-limiting toxicity (DLT; grade 3 rash and grade 3 hyperglycemia, respectively) occurred in two of three patients at the dose of KW-2450 25 mg/day plus lapatinib 1500 mg/day and letrozole 2.5 mg/day. "
3.	Breast Neoplasms (Breast Cancer) 01/01/2018 - "Preclinical studies showed KW-2450 and lapatinib act synergistically to induce in vitro apoptosis and inhibit growth of HER2-positive MDA-MB-361 and BT-474 breast cancer cell lines. " 01/01/2018 - "KW-2450 showed synergistic in vitro growth inhibition with letrozole and 4-hydroxytamoxifen in ER-positive MCF-7 breast cancer cells and MCF-7-Ac1 aromatase-transfected MCF-7 cells. " 04/01/2016 - "Single-agent KW-2450 was associated with modest antitumor activity in heavily pretreated patients with solid tumors and is being further investigated in combination therapy with lapatinib/letrozole in patients with human epidermal growth factor receptor 2-postive metastatic breast cancer. " 01/01/2018 - "We investigated the in vitro and in vivo preclinical activity of KW-2450 plus lapatinib and letrozole and conducted a phase I trial of the triple-drug combination in one male and 10 postmenopausal female patients with advanced/metastatic hormone receptor-positive, human epidermal growth factor receptor 2 (HER2)-positive breast cancer. "
4.	Triple Negative Breast Neoplasms 12/01/2015 - "Antitumor Activity of KW-2450 against Triple-Negative Breast Cancer by Inhibiting Aurora A and B Kinases."
5.	Tetraploidy 12/01/2015 - "In cell-cycle analysis, KW-2450 induced tetraploid accumulation followed by apoptosis or surviving octaploid (8N) cells, depending on dose. "

Related Drugs and Biologics

1.	Lapatinib (GW572016)
2.	Letrozole (Femara)
3.	Hormones (Hormone)
4.	Drug Combinations
5.	human ERBB2 protein
6.	ErbB Receptors (EGF Receptor)
7.	Phosphotransferases (Kinase)
8.	Aromatase (CYP19)
9.	afimoxifene (hydroxytamoxifen)

Related Therapies and Procedures

1.	Therapeutics