U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

    {{facet.count}}
    {{facet.count}}

Showing 4161 - 4170 of 4747 results

Status:
Investigational
Source:
NCT00598806: Phase 3 Interventional Completed Bladder Cancer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Targets:


Apaziquone (EOquin, EO9) is an indolequinone that is a bioreductive prodrug and a chemical analog of the older chemotherapeutic agent mitomycin C. In hypoxic cells, such as those on the inner surface of the urinary bladder, apaziquone is converted to active metabolites by intracellular reductases (such as NQO1). The active metabolites alkylate DNA and lead to apoptosis. In animal tumour models, EO9 was inactive against the P388 murine leukaemia but exhibited anti-tumour activity against human tumour xenografts and the generally chemo-resistant murine adenocarcinomas of the colon (MAC) tumours. Initial evidence that in vivo response correlated with NQO1 activity. Apaziquone was selected for clinical evaluation based upon its novel mechanism of action (which was distinct from MMC), its preferential activity against cells derived from solid tumours in vitro and in vivo, its ability to target both aerobic and hypoxic cells and the lack of myelosuppression in mice and rats. Apaziquone has been applied in clinical studies sponsored by Spectrum Pharmaceuticals and Allergan, Inc. for the treatment of superficial (non-muscle invasive) bladder cancer. However, the US-FDA determined that it was not statistically effective.
Status:
Investigational
Source:
NCT02719977: Phase 1 Interventional Completed Cancer
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

CX-5461 represents an innovative-targeted agent with numerous differentiating features when compared to current options for treatment of hematologic cancers. CX-5461 is a first-in-class small molecule inhibitor of RNA polymerase I (Pol I) that triggers the nucleolar stress surveillance pathways to activate p53, without causing direct DNA damage. Molecular studies demonstrate that CX-5461 inhibits the initiation stage of rRNA synthesis and induces both senescence and autophagy, but not apoptosis, through a p53-independent process in solid tumor cell lines. Currently, CX-5461 is in clinical trial for patients with advanced hematological malignancies.
Status:
Investigational
Source:
NCT03166085: Phase 1 Interventional Completed Metastatic Breast Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



PU-H71 is experimental inhibitor of Hsp90. It is being tested in clinical trials against lymphoma and solid tumors.
Status:
Investigational
Source:
NCT03166085: Phase 1 Interventional Completed Metastatic Breast Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



PU-H71 is experimental inhibitor of Hsp90. It is being tested in clinical trials against lymphoma and solid tumors.
Status:
Investigational
Source:
NCT03166085: Phase 1 Interventional Completed Metastatic Breast Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



PU-H71 is experimental inhibitor of Hsp90. It is being tested in clinical trials against lymphoma and solid tumors.
Status:
Investigational
Source:
NCT01038804: Phase 2 Interventional Completed Breast Cancer
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Sepantronium bromide (YM155) is a selective survivin suppressant that exhibits potent antitumor activities by inducing apoptosis and autophagy in various types of cancer. Sepantronium bromide inhibited the growth of various human cancer cell lines in vitro with GI50 values in the low nM range. Sepantronium bromide blocked the growth of 119 human cancer cell lines, with the greatest inhibition in lines derived from non-Hodgkin's lymphoma, hormone-refractory prostate cancer, ovarian cancer, sarcoma, non-small-cell lung cancer, breast cancer, leukemia, and melanoma, with an average GI50 of 15 nM. Sepantronium bromide inhibited the growth of tumor cell lines regardless of their p53 status and demonstrated significant antitumor activity in 5 mice xenograft models. It also caused tumor regressions in vivo, possibly by its effects in reducing intratumoral survivin expression levels and increasing apoptosis. Sepantronium Bromide had been in phase II clinical trials by Astellas for the treatment of prostate cancer, melanoma, non-Hodgkin's lymphoma, breast cancer, diffuse large B cell lymphoma, non-small cell lung cancer (NSCLC) and other solid tumors. This compound had also been in clinical trials by National Cancer Institute (NCI) for the treatment of solid tumors (phase I) and advanced non-small cell lung cancer (NSCLC) (phase II). However, all these researches about this compound for all indications were discontinued.
Rubitecan [Orathecin™] is a topoisomerase I inhibitor extracted from the bark and leaves of the Camptotheca acuminata tree, which is native to China. Rubitecan is an oral compound being developed for the treatment of pancreatic cancer and other solid tumours by SuperGen. Rubitecan binds to and inhibits the enzyme topoisomerase I and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells; this agent also prevents repair of reversible single-strand DNA breaks.
Status:
Investigational
Source:
NCT03166085: Phase 1 Interventional Completed Metastatic Breast Cancer
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



PU-H71 is experimental inhibitor of Hsp90. It is being tested in clinical trials against lymphoma and solid tumors.
Status:
Investigational
Source:
NCT00486434: Phase 3 Interventional Completed Osteoarthritis
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT03599284: Phase 2 Interventional Completed Coronary Artery Disease
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Showing 4161 - 4170 of 4747 results