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Restrict the search for
m nalidixic acid
to a specific field?
Class (Stereo):
CHEMICAL (ABSOLUTE)
As a narcotic antagonist similar in action to naloxone, DIPRENORPHINE is used to remobilize animals after analgesia by super-potent opioid analgesics such as etorphine and carfentanil. It is not used in humans. Diprenorphine binds approximately equally to the three subtypes of opioid receptors (mu, delta, and kappa) and antagonizes them. This compound belongs to the class of organic compounds known as phenanthrenes and derivatives. These are polycyclic compounds containing a phenanthrene moiety, which is a tricyclic aromatic compound with three non-linearly fused benzene. The therapeutic efficacy of many other compounds can be decreased when used in combination with Diprenorphine (54 compounds mentioned on www.drugbank.ca).
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Pleuromulin (pleuromulitin) is a natural antibiotic isolated from Basidiomycete Pleurotus. Pleuromulitin exhibits activity mainly against gram-positive bacteria including S. aureus, Klebasiella pneumoniae and Bacillus Subtilis. Pleuromulin is an organic compound which is not reported to be used in as a drug however its derivatives have been used in treatment of infections. The first pleuromulitin that was approved in 1979 for use in veterinary medicine was semi-synthetic derivative tiamulin. Semisynthetic pleuromutilin retapamulin (ALTABAX, GlaxoSmithKline) was the first approved for topical use in humans in 2007. Another derivative of pleuromulin, Lefamulin has been successfully tested in phase 1 clinical trial for systemic use in patients (Nabriva Therapeutics AG).
Class (Stereo):
CHEMICAL (ABSOLUTE)
Pinolcaine is 10-methyl-2-substituted piperidine. Pinolcaine is a local anesthetic.
Status:
Investigational
Source:
NCT00116610: Phase 2 Interventional Completed Small Cell Lung Cancer
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Picoplatin is a sterically hindered platinum (II) complex with antineoplastic properties developed for the treatment of cis-platin-resistant cancer. Picoplatin alkylates DNA, forming both inter- and intra-strand cross-linkages, resulting in inhibition of DNA replication and transcription, and the induction of apoptosis. However, in Phase III trials, picoplatin failed to meet its primary endpoint for advanced cell lung cancer. It remains in development for other cancers.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Mivobulin is a synthetic water-soluble colchicine analog with the broad antitumor activity that competitively binds tubulin at the colchicine-binding site and inhibits tubulin polymerization. Cancer cells exposed to Mivobulin isethionate accumulate in the M phase of the cell cycle and subsequently die. Preclinical studies have demonstrated that Mivobulin isethionate is able to cross the blood-brain barrier. Importantly, Mivobulin isethionate demonstrated significant antitumor activity in a broad spectrum of murine and human tumor models that were cross-resistant to vincristine, cisplatin, vinblastine, navelbine, and doxorubicin and in tumor cell lines exhibiting multidrug resistance owing to P-glycoprotein overexpression. In animal studies, the activity of Mivobulin isethionate was largely independent of the route of drug administration but favored a prolonged treatment schedule. Unfortunately, in clinical trials, Mivobulin fail to demonstrate the significant activity
Status:
Investigational
Source:
NCT04669587: Phase 1/Phase 2 Interventional Unknown status Estrogen Receptor-Positive
(2021)
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Adaprolol is a beta-adrenergic antagonist that is being developed as a topical agent to treat glaucoma. Adaprolol demonstrated a safer cardiovascular profile, especially in the population over 70 years old. It was in Phase II clinical trials for the treatment of glaucoma. This research has been discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Daltroban (also known as BM 13505, SKF 96148), a specific thromboxane A2 receptor antagonist, was studied as an antithrombotic agent. The drug was licensed to Smith Kline Beecham, underwent phase III clinical trials in the UK and Germany as an antithrombotic agent but did not enter clinical trials in the USA. Besides, вaltroban was investigated in patients with an ischemic heart disorder. However, the development of daltroban has been discontinued.
Status:
Investigational
Source:
NCT00664378: Phase 2 Interventional Terminated Relapsed and Refractory Multiple Myeloma
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
CYT997 (Lexibulin) is a wholly synthetic compound that possesses highly potent cytotoxic activity in vitro through inhibition of microtubule polymerization. CYT997 (Lexibulin) is a potent microtubule polymerization inhibitor with IC50 of 10-100 nM in cancer cell lines. CYT997 (Lexibulin) blocks the cell cycle at the G(2)-M boundary, and Western blot analysis indicates an increase in phosphorylated Bcl-2, along with increased expression of cyclin B1. Caspase-3 activation is also observed in cells treated with CYT997 (Lexibulin) along with the generation of poly(ADP-ribose) polymerase. The compound possesses favorable pharmacokinetic properties, is orally bioavailable, and is efficacious per os in a range of in vivo cancer models, including some refractory to paclitaxel treatment. CYT997 (Lexibulin) exhibits vascular disrupting activity as measured in vitro by effects on the permeability of human umbilical vein endothelial cell monolayers, and in vivo by effects on tumor blood flow. CYT997 (Lexibulin) possesses a useful combination of pharmacologic and pharmacokinetic properties having considerable potential as a novel anticancer agent. Lexibulin was being developed by YM BioSciences as a vascular-disrupting agent (VDA) for the potential treatment of cancer, it was in phase II development on YM BioSciences ' pipeline. It appears that the development of lexibulin has been discontinued.
Status:
Investigational
Source:
NCT02223481: Phase 2 Interventional Completed Hypertension, Pulmonary
(1998)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Terbogrel, an agent having two pharmacodynamic actions, namely inhibition of thromboxane A2 synthase and antagonism of the thromboxane A2 receptor. The antithrombotic effect of terbogrel was dose-dependent and was associated with enhanced prostacyclin production. The drug was studied for the treatment of peripheral vascular disorders, pulmonary hypertension, and thrombosis. Terbogrel participated in phase II clinical trial to investigate its safety and efficacy in patients with primary pulmonary hypertension, however, this study was discontinued due to terbogrel’s induction of leg pain.
