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

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Showing 131 - 140 of 5943 results

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

Class (Stereo):
CHEMICAL (UNKNOWN)

Lemuteporfin is a newly introduced, light-sensitive drug for use in combination photodynamic therapy (PDT). It acts on mitochrondria to initiate the apoptotic cascade resulting in cell death (apoptosis). The photosensitizer was highly potent, killing cells at low nanomolar concentrations upon exposure to activating light. The cellular uptake of lemuteporfin was rapid with maximum levels reached within 20 min. Mitogen-activated lymphoid cells accumulated more of the lemuteporfin than their quiescent equivalents, supporting selectivity. Lemuteporfin had been in phase II clinical trials for the treatment of benign prostatic hypertrophy. It is in phase I clinical trials for the treatment of acne rosacea.
Status:
Investigational
Source:
INN:lirafugratinib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:losoxantrone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Losoxantrone is an anthrapyrazole that induces both single and double strand breaks in DNA and is a potent inhibitor of DNA synthesis. The drug is in clinical trials for the treatment of breast cancer and of prostate cancer that is refractory to androgen ablation. Acute toxicity is negligible. Losoxantrone may be less cardiotoxic than doxorubicin. Up to 40% of patients encounter alopecia. 3% of patients develop congestive heart failure. Losoxantrone had been in phase II clinical trial for the treatment of breast and prostate cancer. However, this development was discontinued.
Status:
Investigational
Source:
INN:encyprate [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Encyprate (MO-1255) is a unique drug in being inactive as an MAO inhibitor in vitro but very active in vivo. It most probably is converted by the body to ethyl-N-benzyl-N-cyclopropylcarbamate which is an active MAOI in vitro. I was studying in the treatment of depression.
Status:
Investigational
Source:
INN:nezulcitinib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)



Veliflapon (BAY X1005, DG-031) is an enantioselective inhibitor of 5-lipoxygenase activating protein, or FLAP. There are variants in the gene encoding FLAP, and the gene encoding leukotriene A4 hydrolase (LTA4H) linked to risk of heart attack. These variants appear to confer increased risk of heart attack by increasing the production of leukotriene B4 (LTB4), a potent driver of inflammation produced in atherosclerotic plaques. deCODE licensed veliflapon (BAY X1005, DG-031) from Bayer AG, which developed it originally for the treatment of asthma.
Status:
Investigational
Source:
INN:luvadaxistat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:trospectomycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trospectomycin is an aminocyclitol antibiotic similar in structure to spectinomycin. The drug was originally developed by Pharmacia & Upjohn. It is a 6'-propyl analogue of spectinomycin, and lacks the aminosugars in glycosidic linkage which are thought to be responsible for the ototoxicity and nephrotoxicity associated with the aminoglycosides. The mechanism of action of trospectomycin is similar to that of its parent compound, spectinomycin: it binds to the bacterial 30S ribosome and inhibits protein synthesis. The transport mechanism for its delivery to its target site does not appear to be oxygen dependent, and this explains the in-vitro activity of trospectomycin against anaerobic organisms. Trospectomycin has activity against a broad spectrum of pathogenic organisms including Streptococcus, Haemophilus, Gardnerella, Neisseria, Peptococcus, Peptostreptococcus, Bacteroides, Mobiluncus, Chlamydia, Mycoplasma and Ureaplasma spp. Results of in-vivo testing suggest potential utility in a variety of clinical conditions including non-gonococcal urethritis, chlamydial cervicitis, gonorrhoea, pelvic inflammatory disease, pneumonia, anaerobic infections and meningitis. Trospectomycin progressed to late stage clinical trials for treatment of pelvic inflammatory disease (chlamydia) before being abandoned for commercial reasons as the third generation cephalosporins and second generation macrolides in development and use were judged superior at the time.
Status:
Investigational
Source:
INN:vidupiprant [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Vidupiprant, also known as AMG 853, is an orally bioavailable and potent dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors. Vidupiprant inhibits PGD2-induced down modulation of CRTH2 on CD16- granulocytes in human whole blood as well as PGD2-induced cAMP response in platelets. It inhibits PGD2-induced airway constriction in vivo. Also inhibits BRD4 (Kd = 170 nM). AMG 853 as an add-on to inhaled corticosteroid therapy demonstrated no associated risks but was not effective at improving asthma symptoms or lung function in patients with inadequately controlled moderate-to-severe asthma. AMG 853 has been discontinued due to poor efficacy.
Status:
Investigational
Source:
INN:flucrilate [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

FLUCRYLATE, fluoroalkyl cyanoacrylate, is a surgical tissue adhesive.