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

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Showing 741 - 750 of 24423 results

Status:
Investigational
Source:
NCT01082471: Phase 3 Interventional Completed Postoperative Pain
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Morphine-6-glucuronide is a pharmacologically active metabolite of morphine that is being developed by CeNeS Pharmaceuticals as an alternative to morphine for the management of postoperative pain. Compared to morphine, Morphine-6-glucuronide has been reported to have6 and 86 times lower affinity for the human mu and kappa opioid receptors, respectively, and similar affinity for the delta opioid receptor. Morphine-6-glucuronide is was studied in phase III clinical trials for postoperative pain management. Unfortunately, Morphine-6-glucuronide failed to demonstrate superior safety compared to Morphine and further development was discontinued. Morphine-6-glucuronide accumulates after administration of morphine to patients with renal insufficiency, and analgesia can be obtained with lower doses of morphine compared to patients with normal renal function. More importantly, the dose should be reduced to avoid serious side-effects, although the simulations in this review did not account for side-effects.
Status:
Investigational
Source:
NCT00134199: Phase 2/Phase 3 Interventional Completed Obesity
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Otenabant (CP-945,598) is Pfizer developed as a potent and selective cannabinoid receptor CB1 antagonist with Ki of 0.7 nM, which exhibits 10,000-fold greater selectivity against human CB2 receptor, for treatment of obesity. In clinical trial III Pfizer decided to discontinue the development program based on changing regulatory perspectives on the risk/benefit profile of the CB1 class and likely new regulatory requirements for approval.
Status:
Investigational
Source:
INN:rafigrelide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Rafigrelide is an imidazoquinazoline derivative patented by pharmaceutical company Shire LLC as platelet-lowering agent for the treatment of myeloproliferative diseases. Rafigrelide is a chemical analog of anagrelide, which is used to reduce platelet counts in myeloproliferative disorders. Compared with anagrelide, Rafigrelide has reduced potency against phosphodiesterase III, which may help to reduce potential side effects. The concentration of Rafigrelide that produces 50% of the maximum inhibition (IC50) of PDE III is 164 nM, making it an approximately 200-fold less potent inhibitor of phosphodiesterase III than 3-hydroxy anagrelide. In the clinical trial, Rafigrelide showed antithrombotic properties during a two-week treatment period in healthy male volunteers. The reductions in thrombus formation were seen in surrogate models of both high and low shear rates suggesting drug efficacy in different arterial conditions.
Status:
Investigational
Source:
NCT03756103: Phase 2 Interventional Completed Hypertension,Essential
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT04323124: Phase 1 Interventional Terminated Healthy
(2020)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT02753699: Phase 3 Interventional Completed Hepatitis C
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Alisporivir (DEBIO-025) is a first-in-class synthetic cyclophilin inhibitor, in development with Debiopharm as an oral treatment for hepatitis C virus (HCV) infections. Alisporivir has the potential to be used for the treatment of additional diseases such as other viral infections, certain muscular dystrophies, and myocardial infarction. Alisporivir has potent anti-hepatitis C virus (HCV) activity both in vitro and in vivo. It is currently being evaluated in phase II clinical trials.
Status:
Investigational
Source:
Inhal Toxicol. 2015;27(14):810-21.: Not Applicable Human clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

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

Class (Stereo):
CHEMICAL (RACEMIC)

ISOMETHADONE HYDROBROMIDE, DL- is a hydrobromide salt of isomethadone, a synthetic opioid analgesic. This is a controlled substance in the US.
Status:
Investigational
Source:
NCT03285711: Phase 2 Interventional Completed Lupus Membranous Nephropathy
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)