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

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Showing 11401 - 11410 of 13268 results

Status:
Investigational
Source:
NCT00832546: Phase 1 Interventional Completed Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Tezampanel, also known as LY 293558 and NGX-424, is a drug originally developed by Eli Lilly, which is a competitive antagonist of the AMPA and kainate subtypes of the ionotropic glutamate receptor family. Tezampanel was in phase II clinical trial for treatment migraine, but this study was discontinued. Also this drug has several others potential pharmacological actions, one of them is anxiety disorders
Status:
Investigational
Source:
INN:dagapamil
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Dagapamil is a calcium-channel blocker, discovered by BASF. The compound is claimed to have antihypertensive, antiarrhythmic, cardioprotective, antiallergic and platelet aggregation-inhibiting action in animal models.
Status:
Investigational
Source:
NCT01423851: Phase 1/Phase 2 Interventional Completed Primary Myelofibrosis
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


NS-018 is a potent inhibitor of Janus kinase 2 (JAK2) enzyme activity and Src-family kinases. It was developed as an oral therapy for the treatment of myelofibrosis. Overall NS-018 has been used in trials studying the treatment of primary myelofibrosis, post-polycythemia vera myelofibrosis, and post-essential thrombocythemia. NS-018 is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). NS-018 also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. NS-018 shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene.
Status:
Investigational
Source:
INN:dexlofexidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Dexlofexidine is an isomer “+“ of lofexidine, which is agonist of alpha 2-adrenoceptor, but in 10 times less potent than the other isomer, levlofexidine.
Status:
Investigational
Source:
NCT04712669: Phase 2 Interventional Completed Pulmonary Arterial Hypertension
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:fenpipalone [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

FENPIPALONE is an oxazolidinone derivative with central nervous system depressant and antiinflammatory activity in animal models. However, FENPIPALONE did not demonstrate any usefulness for severely ill chronic schizophrenic patients.
Vanoxerine, also known as GBR-12909, is a piperazine derivative exhibiting potent selective inhibition of sodium-dependent dopamine reuptake transporters. Vanoxerine has been in clinical trials for Parkinsonism, depression and cocaine addiction but lacked efficacy. Vanoxerine has also been observed as a potent blocker of the following channels: cardiac hERG/IKr potassium channel, Calcium channel, voltage-dependent, L type, alpha 1C subunit (also known as Cav1.2) and voltage-gated sodium channel Nav 1.5. Vanoxerine was studied as a potential treatment for atrial fibrillation. However, phase III clinical trials for this condition were terminated because of cardiac safety concerns. Research also indicates that vanoxerine may have additional mechanisms of action including antagonist action at nicotinic acetylcholine receptors (nAChRs).
Status:
Investigational
Source:
INN:furethidine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:flumecinol [INN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)


FLUMECINOL, a benzhydrol derivative, is a hepatic microsomal drug-metabolizing enzyme inducer. It was in clinical development for the treatment of pruritus associated with primary biliary cirrhosis.
Status:
Investigational
Source:
NCT04035473: Phase 1 Interventional Completed Solid Tumor
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



HM-30181 is a highly selective and potent inhibitor of Multi-drug resistance 1 (MDR1, ABCB1), also known as P-glycoprotein (P-gp). Co-administration of HM30181 greatly increased oral bioavailability of tubulin-stabilizing chemotherapeutic agent paclitaxel. Oraxol is an oral dosage form of paclitaxel administered orally with the HM30181A molecule. Oraxol offers patients with paclitaxel-responsive tumors the possibility of oral therapy without the requirement for premedication to prevent infusion-related hypersensitivity-type reactions. Current clinical data suggests the promising potential of a better clinical response and tolerability profile, which can likely to be attributed to the better pharmacokinetic profile achieved. Oraxol is presently in a Phase 3 trial in metastatic breast cancer and poised to enter into a combination study for treatment of advanced gastric cancer with ramucirumab through a clinical trial collaboration with Eli Lilly and Company.

Showing 11401 - 11410 of 13268 results