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

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Showing 981 - 990 of 13408 results

Status:
Investigational
Source:
INN:afeletecan
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Afeletecan (Bay 38-3441) is a camptothecin glycoconjugate which stabilizes the active lactone form of camptothecin and allows selective uptake into tumor cells. Afeletecan is a topoisomerase inhibitor. Afeletecan was in phase I clinical trials with Bayer for the treatment of cancer; however, development appears to have been discontinued.
Status:
Investigational
Source:
INN:alestramustine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Alestramustine is the l-alanine ester form of estramustine, a combination of the nitrogen mustard normustine coupled via a carbamate to estradiol, with antineoplastic activity. Upon conversion of alestramustine to estramustine, estramustine binds to microtubule-associated proteins (MAPs) and beta tubulin, thereby interfering with microtubule dynamics and leading to microtubule disassembly and cell cyle arrest. Due to the estrogen moiety, this agent is able to selectively bind to and be taken up by estrogen receptor-positive cells.
Status:
Investigational
Source:
INN:ciladopa
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Ciladopa, is a troponylpiperazine derivative and dopamine agonist that has been shown to influence dopaminergic mechanisms in animals. Preclinical pharmacological studies have suggested that it has antiparkinsonian activity similar to that of bromocriptine but without many of the troublesome side effects. Unfortunately in some clinical trials no significant differences was found among the treatment groups and placebo.
Losmapimod (GW856553, GSK-AHAB) is a selective, potent, and orally active p38 MAPK (p38α and p38β isoforms) inhibitor that acts by competing for the kinase ATP binding site. GlaxoSmithKline (GSK) is developing oral losmapimod for the treatment of acute coronary syndromes (phase III), chronic obstructive pulmonary disease (phase II) and primary focal segmental glomerulosclerosis (phase II). Oral losmapimod was in phase II development for the treatment of rheumatoid arthritis and major depressive disorder; however, it appears that development for these indications has been discontinued. No further development was reported for atherosclerosis, dyslipidaemia and neuropathic pain.
AT-9283 was being developed by Astex Pharmaceuticals as a treatment for cancer and myelofibrosis. AT-9283 is an inhibitor of mitosis (cell division) and is the second most progressed drug candidate in the Astex portfolio of novel molecularly targeted cancer drugs. All of Astex’s current products have been discovered internally using its proprietary drug discovery approach. AT9283 is a potent inhibitor of the Aurora A and B kinases and has been shown to arrest tumour growth in a range of tumour models. Aurora kinases play a key role in mitotic checkpoint control in cell division. Both Aurora A and B are over-expressed in many human tumours and are believed to be excellent targets for anti-cancer therapy.
Status:
Investigational
Source:
INN:pyrrolifene [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Pyrroliphene is a dialkylaminodiphenylbutanol ester with antitussive and analgesic activities. In clinical trials the major side effect of Pyrroliphene was sedation, and the other side effect liabilities were similar to those of morphine.
Status:
Investigational
Source:
INN:trigevolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Trigevolol is a beta-adrenergic blocking agent. It was developed as an antiarrhythmic and antihypertensive drug.
Status:
Investigational
Source:
INN:enadoline
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Enadoline (CI-977) is a potent and selective agonist at the kappa-opioid receptor. Enadoline is a potent antinociceptive agent. Clinical use of enadoline was associated with dose-limiting neuropsychiatric adverse events. Enadoline may yet find some application against ischaemic stroke and severe head injury, presumably in comatose patients.
Status:
Investigational
Source:
INN:cefdaloxime [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefdaloxime is a third-generation cephalosporin antibiotic patented by pharmaceutical company Roussel-UCLAF. Cefdaloxime activity was the poorest among the different oral cephalosporins.
Status:
Investigational
Source:
INN:flortanidazole (¹⁸F) [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

FLORTANIDAZOLE F-18 is a radioactive tumor hypoxia tracer to potentially identify and quantify the degree of hypoxia in tumors in vivo via positron emission tomography (PET) imaging.