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

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Showing 11481 - 11490 of 13268 results

Status:
Investigational
Source:
NCT03301454: Phase 2 Interventional Unknown status Esophageal Cancer, Squamous Cell
(2018)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Imazethapyr is an imidazole compound used as a selective herbicide. It is applied preplant incorporated, preemergence, at cracking, and postemergence. The compound controls weeds by reducing the levels of three branched-chain aliphatic amino acids, isoleucine, leucine and valine, through the inhibition of aceto-hydroxyacid synthase, an enzyme common to the biosynthetic pathway for these amino acids. This inhibition causes a disruption in protein synthesis which, in turn, leads to an interference in DNA synthesis and cell growth. The compound is used to control grasses and broadleaved weeds including barnyardgrass, crabgrass, cocklebur, panicums, pigweeds, nightshade, mustard, smartweed, velvetleaf, jimsonweed, foxtails, seedling johnsongrass, lambsquarters, morningglory and others. Tolerant crops include soybeans, peanuts, dry and edible beans, peas, alfalfa and imidazolinone resistant/tolerant corn. Additional research is being conducted on other leguminous crops. Acetolactate synthase inhibition is the primary mechanism of action of imazethapyr (IM).
Status:
Investigational
Source:
NCT04663308: Phase 2 Interventional Recruiting Primary Sclerosing Cholangitis
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Volixibat (SHP626; formerly LUM002) is a potent inhibitor of the apical sodium-dependent bile acid transporter (ASBT) that was developed for the treatment of nonalcoholic steatohepatitis. Volixibat participated in phase II clinical trial to investigate its safety, effectiveness in adults with nonalcoholic steatohepatitis. However, this study was discontinued, without any further explanation for the possible causes. In addition, volixibat was studied in a clinical trial in healthy adults and in patients with type 2 diabetes mellitus, where was shown that the drug was generally well tolerated.
Status:
Investigational
Source:
NCT03563599: Phase 2 Interventional Completed Treatment-naïve, Sputum Smear-positive Patients With Drug-sensitive Pulmonary TB
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Q203 (6-chloro-2-ethyl-N-(4-(4-(4-(trifluoromethoxy)phenyl)piperidin-1-yl)benzyl)imidazo [1,2-a]pyridine-3-carboxamide) is an an imidazopyridine antitubercular compound. Q203 targets the cytochrome b subunit (QcrB) of the cytochrome bc1 complex. This complex is an essential component of the respiratory electron transport chain of ATP synthesis. Q203 inhibited the growth of multidrug-resistant (MDR) and extensively drug-resistant (XDR) M. tuberculosis clinical isolates in culture broth medium in the low nanomolar range and was efficacious in a mouse model of tuberculosis at a dose less than 1 mg per kg body weight, which highlights the potency of this compound. In addition, Q203 displays pharmacokinetic and safety profiles compatible with once-daily dosing. Q203 is a promising new clinical candidate for the treatment of tuberculosis.
Status:
Investigational
Source:
NCT04395677: Phase 2 Interventional Active, not recruiting Non Small Cell Lung Cancer
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:etoxeridine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Etoxeridine (Carbetidine or Wy2039), a piperidine derivative, is a narcotic analgetic.
Status:
Investigational
Source:
NCT00329368: Phase 1 Interventional Completed Cancer
(2005)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
INN:fosopamine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Epinine or deoxyepinephrine is an active form of Ibopamine, which is used as a cardiovascular agent in congestive heart failure. Epinine is a stimulant of alpha-adrenoceptor activities: alpha-1 and alpha-2. Experiments on pig’s eyes have shown that epinine can be a promising candidate substance for intraoperative (e.g., cataract surgery) intracameral use in humans.
Status:
Investigational
Source:
INN:pentopril
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pentopril (CGS 13945) is a member of a series of l-glutarylindoline-2(S)-carboxylic acid derivatives. Pentopril was evaluated as an inhibitor of a cell-free preparation of angiotensin-converting enzyme (ACE) isolated from rabbit lung. Intravenous administration of incremental doses of pentopril to anesthetized normotensive rats produced a dose-related inhibition of angiotensin I (AI) pressor responses. The onset of inhibition of the A1 pressor response was rapid, and substantial inhibition occurred at 5 min after administration of the ACE inhibitors. Pentopril hydrolyzed in vivo to the biologically active free-acid form of CGS 13934. It was well tolerated in normal volunteers and hypertensive patients. Pentopril was developed for the treatment of both hypertension and congestive heart failure. Pentopril produced little clinical improvement and no biochemical improvement in a patients with rheumatoid arthritis.
Status:
Investigational
Source:
NCT03098979: Phase 2 Interventional Completed Heart Failure
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Neladenoson bialanate (BAY1067197) is the first oral partial and highly selective A1R agonist that has entered clinical development for the treatment of heart failure. Neladenoson bialanate maintains the cardioprotective effects of adenosine without the undesired side effects of a full agonist. Of particular importance in this clinical development is the potential influence of concomitant use of β-blockers as they have the potential to increase the risk of AV conduction abnormalities with A1R agonist treatment. Two small phase 2a pilot studies evaluating the short-term safety of neladenoson bialanate in patients with HFrEF pretreated with β-blockers have recently completed, and the results are pending (ClinicalTrials.gov identifiers: NCT02040233 and NCT01945606). In a small phase 1 trial in healthy volunteers pretreated with the β-blocker metoprolol succinate, a single 50 mg oral dose of neladenoson bialanate administered together with metaprolol succinate was found to be well tolerated. Notably, no higher degree AV block, prolongation of the PR interval, or relevant decreases in heart rate or systemic blood pressure were observed.
Status:
Investigational
Source:
NCT03701295: Phase 1/Phase 2 Interventional Completed Acute Myeloid Leukemia With t(9;11)(p21.3;q23.3); MLLT3-MLL
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Pinometostat, also known as EPZ-5676, is a small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Upon intravenous administration, EPZ-5676 specifically blocks the activity of the histone lysine-methyltransferase DOT1L, thereby inhibiting the methylation of nucleosomal histone H3 on lysine 79 (H3K79) that is bound to the mixed lineage leukemia (MLL) fusion protein which targets genes and blocks the expression of leukemogenic genes. Epizyme is developing pinometostat, a small molecule inhibitor of DOT1L, for the treatment of patients with MLL-r, a genetically defined acute leukemia. Epizyme is conducting a phase 1 clinical trial in pediatric patients. Epizyme is evaluating preclinical combinations of pinometostat with other anti-cancer agents in MLL-r leukemia. Pinometostat is being developed in collaboration with Celgene. Epizyme retains all U.S. rights to pinometostat and has granted Celgene an exclusive license to pinometostat outside of the U.S.

Showing 11481 - 11490 of 13268 results