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Restrict the search for
m tamoxifen
to a specific field?
Status:
Investigational
Source:
NCT00427856: Phase 2 Interventional Completed Lymphoma, Follicular
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Obatoclax (GX15-070) is a novel BH3 mimetic pan Bcl-
2 inhibitor. The clinically studied formulation is as obatoclax mesylate (Box 1), a salt. It is only under study as an intravenous preparation. It functions to block BH3-mediated binding of Bcl-2, Bcl-XL, Mcl-1 and A1 to Bax and Bak. Bax and Bak thus are unopposed and able to dimerize to allow initiation of intrinsic apoptosis. Preclinically, obatoclax has been shown to reverse inhibition of Bax or Bak by Bcl-2, Bcl-XL, Bcl-w and Mcl-1. Obatoclax was discovered by Gemin X, which was acquired by Cephalon, which has since been acquired by Teva Pharmaceuticals. Obatoclax had been in phase III clinical trials by Gemin X Biotechnologies (subsidiary of Teva) for the treatment of non-small lung cancer (NSCLC).
The compound received orphan drug designation in the U.S. in 2004 for the treatment of chronic lymphocytic leukemia (CLL). However, Teva discontinued the development of obatoclax in 2013.
Status:
Investigational
Source:
NCT01640808: Phase 3 Interventional Completed Hepatic Neoplasm Malignant Recurrent
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Peretinoin is an orally available, acyclic retinoid with potential antineoplastic and chemopreventive activities. Peretinoin binds to and activates nuclear retinoic acid receptors (RAR), which in turn recruit coactivator proteins and promote, with other transcriptional complexes, the transcription of target genes. As a result, this agent may modulate the expression of genes involved in the regulation of cell proliferation, cell differentiation, and apoptosis of both normal and tumor cells. Peretinoin inhibits post-therapeutic recurrence of hepatocellular carcinoma via unclear mechanisms. The European Commission granted Orphan Drug designation for Kowa's peretinoin to treat hepatocellular carcinoma (HCC).
Status:
Investigational
Source:
NCT02535312: Phase 1/Phase 2 Interventional Active, not recruiting Advanced Malignant Solid Neoplasm
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Methoxyamine (TRC102) is an orally bioavailable small molecule with potential adjuvant activity, that may potentiate the antitumor activity of alkylating agents. Methoxyamine covalently binds to apurinic/apyrimidinic (AP) DNA damage sites and inhibits base excision repair (BER) that causes topoisomerase II-dependent irreversible strand breaks and apoptosis. Methoxyamine is currently being studied in multiple Phase 1 and Phase 2 clinical trials sponsored by the National Cancer Institute or Case Comprehensive Cancer Center.
Class (Stereo):
CHEMICAL (RACEMIC)
Class (Stereo):
CHEMICAL (ABSOLUTE)
Homprenorphine is an opioid receptor agonist with opioid analgesic activity. This compound has never been marketed.
Status:
Investigational
Source:
NCT01314014: Phase 2 Interventional Completed Follicular Lymphoma
(2011)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Imexon (INN, trade name Amplimexon) is a substance that is being studied in the treatment of some types of cancer, including pancreatic, lung, breast, prostate, melanoma, and multiple myeloma. Imexon is a thiol-binding small molecule which induces mitochondrial oxidation, a loss of membrane potential and cytochrome C, leading to apoptosis.
Status:
Investigational
Source:
NCT00806338: Phase 1 Interventional Completed Diabetes Mellitus
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Trodusquemine (MSI-1436) is a "first-in-class" highly selective non-competitive, allosteric inhibitor of PTP1B that can cross the blood-brain barrier to suppress feeding and promote insulin sensitivity and glycemic control. Trodusquemine is a naturally occurring cholestane that can be purified from the liver of the dogfish shark, Squalus acanthias, but it can also be manufactured synthetically by a fairly laborious process that requires several weeks. Trodusquemine has potential hypoglycemic, anti-diabetic, anti-obesity, and antineoplastic activities. Upon administration, trodusquemine selectively targets and inhibits PTP1B, thereby preventing PTP1B-mediated signaling. This prevents the dephosphorylation of the insulin receptor, which improves insulin signaling and insulin sensitivity, and decreases blood glucose levels. In susceptible cancer cells, inhibition of PTP1B causes a reduction of tumor cell proliferation.
Status:
Investigational
Source:
NCT00659490: Phase 2 Interventional Completed Pain
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01113970: Phase 1/Phase 2 Interventional Unknown status Metastatic Breast Cancer
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Indibulin is a novel synthetic compound that was identified in a cell-based screening assay to discover cytotoxic drugs. Indibulin destabilizes microtubules and blocks cell cycle transition specifically at the G2-M phase. Indibulin effectively induces apoptosis through Bcl-2 phosphorylation and Bax translocation in human malignant glioma cells in a p53-independent manner. This agent has been shown to be active against multidrug-resistant (MDR) and taxane-resistant tumour cell lines. Indibulin was used in phase I/II clinical trials of patients with advanced solid tumours (metastatic breast cancer). Pharmacokinetic analysis showed a better tolerability underfeeding condition. Dose-limiting toxicities were nausea and vomiting, which seemed to be related to solvent lactic acid.
Class (Stereo):
CHEMICAL (ACHIRAL)
Cilutazoline is phenoxymethyl-imidazoline derivative useful as cardiotonics and vasoconstrictors
