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Restrict the search for
phenyl aminosalicylate
to a specific field?
Status:
Investigational
Source:
INN:locnartecan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT03750552: Phase 3 Interventional Completed Symptomatic Neurogenic Orthostatic Hypotension
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00619164: Phase 2 Interventional Completed Acute Coronary Syndrome
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Atopaxar, also known as E 5555 is a novel reversible protease-activated receptor-1 (PAR-1) thrombin receptor antagonist. The inhibition of thrombin-mediated platelet activation by means of protease-activated receptor-1 inhibitors represents an attractive therapeutic option for patients with atherothrombotic disease processes. In preclinical studies, atopaxar demonstrated inhibition of thrombin receptor-activating peptides (TRAP)- and thrombin-induced platelet aggregation. Atopaxar was being developed by Eisai for acute coronary syndromes (ACS) and coronary disorders, including atherothrombosis, unstable angina pectoris and myocardial infarction. Atopaxar was in phase II clinical development in the US, EU and Japan. However, development was discontinued in May 2012.
Status:
Investigational
Source:
NCT04696848: Phase 1/Phase 2 Interventional Terminated Colorectal Cancer
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
CKD-516 is a prodrug of the tubulin binding agent S516, with potential tubulin-inhibiting, vascular-disrupting, and antineoplastic activity. Upon administration, tubulin polymerization inhibitor CKD-516 is converted into its active metabolite S-516, which binds to tubulin and prevents its polymerization in tumor blood vessel endothelial cells and tumor cells. This blocks the formation of the mitotic spindle and leads to cell cycle arrest at the G2/M phase. As a result, this agent disrupts the tumor vasculature and tumor blood flow, deprives tumor cells of nutrients and induces tumor cell apoptosis. In addition, this agent has a direct cytotoxic effect on tumor cells by inhibiting tubulin polymerization. CKD-516 is developed by a Korean company Chong Kun Dang Pharmaceutical Corp. and is investigated in a phase 1/2a clinical trial for the treatment of colorectal cancer in combination with Irinotecan.
Status:
Investigational
Source:
NCT03042013: Phase 2 Interventional Withdrawn Subjects With NSCLC With an EGFR Activating Mutation
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Naquotinib (ASP8273) is an orally available, irreversible, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor, with potential antineoplastic activity. Naquotinib was found by mass spectrometry to covalently bind to a mutant EGFR (L858R/ T790M) via cysteine residue 797 in the kinase domain of EGFR with long-lasting inhibition of EGFR phosphorylation for 24 h. In the NSCLC cell lines harboring the above EGFR mutations, Naquotinib had IC50 values of 8-33 nM toward EGFR mutants, more potently than that of WT EGFR (IC50 value of 230 nM). In mouse xenograft models, Naquotinib induced complete regression of the tumors after 14 days of treatment. ASP8273 even showed activity in mutant EGFR cell line which is resistant to other EGFR TKIs. Naquotinib is in phase III clinical trials for the oral treatment of EGFR mutated non-small cell lung cancer (NSCLC).
Status:
Investigational
Source:
NCT00600275: Phase 1/Phase 2 Interventional Completed Solid Tumors
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
BGT 226 is an orally available, small molecule, the dual inhibitor of mammalian target of rapamycin (mTOR) and phosphatidylinositol 3'kinase (PI3K), developed by Novartis for the treatment of solid tumors, including advanced breast cancer. A phase I/II trial was completed in the US, Canada, and Spain, and a phase I trial was completed in Japan. However, development appears to have been discontinued.
Status:
Investigational
Source:
JAN:LANPERISONE HYDROCHLORIDE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Lanperisone (NK433) is muscle relaxant. It acts by blocking voltage-gated sodium channels.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Ampyrone (4-Aminoantipyrine or AAP) is a metabolite of aminophenazone and is an aromatic substance with analgesic, antipyretic and anti-inflammatory properties. When combined with the antineoplastic agents, ampyrone decreased their genotoxic, mutagenic, apoptotic, and phagocytic effects. However, ampyrone usually produces side effects, such as the risk of agranulocytosis. Although ampyrone is scarcely ever administered as an analgesic because of the potential side effects, as a raw material, it is mostly used to produce ampyrone derivatives, which have better biological activities. In addition, it is used as a reagent for biochemical reactions producing peroxides or phenols and can also be used to detect phenols in the environment. Exposure to ampyrone could induce changes in the enzyme catalase structure and function.
Status:
Investigational
Source:
NCT02311933: Phase 2 Interventional Active, not recruiting Recurrent Breast Carcinoma
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is active metabolites of tamoxifen. This metabolite exhibits a 100-fold higher binding affinity to the estrogen receptor (ER) and are more effective in suppressing cell proliferation than tamoxifen. In humans, the conversion from tamoxifen to endoxifen is predominant. Endoxifenis is an orally active, selective estrogen receptor modulator (SERM) that was developed for the treatment of estrogen receptor-positive breast cancer. In addition, this drug possesses antimanic properties, what can be used in the treatment of patients with bipolar I disorder (BPD I).
Status:
Investigational
Source:
NCT04696848: Phase 1/Phase 2 Interventional Terminated Colorectal Cancer
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
CKD-516 is a prodrug of the tubulin binding agent S516, with potential tubulin-inhibiting, vascular-disrupting, and antineoplastic activity. Upon administration, tubulin polymerization inhibitor CKD-516 is converted into its active metabolite S-516, which binds to tubulin and prevents its polymerization in tumor blood vessel endothelial cells and tumor cells. This blocks the formation of the mitotic spindle and leads to cell cycle arrest at the G2/M phase. As a result, this agent disrupts the tumor vasculature and tumor blood flow, deprives tumor cells of nutrients and induces tumor cell apoptosis. In addition, this agent has a direct cytotoxic effect on tumor cells by inhibiting tubulin polymerization. CKD-516 is developed by a Korean company Chong Kun Dang Pharmaceutical Corp. and is investigated in a phase 1/2a clinical trial for the treatment of colorectal cancer in combination with Irinotecan.
