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

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Showing 11 - 20 of 297 results

Status:
First approved in 1953

Class (Stereo):
CHEMICAL (ABSOLUTE)


Riboflavin (vitamin B2) is part of the vitamin B group. Riboflavin 5’-phosphate is the precursor of two coenzymes, flavin adenine dinucleotide and flavin mononucleotide, which catalyze oxidation/reduction reactions involved in a number of metabolic pathways. FAD and riboflavin phosphate in foods are hydrolyzed in the intestinal lumen by nucleotide diphosphatase and a variety of nonspecific phosphatases to yield free riboflavin, which is absorbed in the upper small intestines by a sodium-dependent saturable mechanism. Riboflavin has been used in several clinical and therapeutic situations. For over 30 years, riboflavin supplements have been used as part of the phototherapy treatment of neonatal jaundice. Corneal ectasia is a progressive thinning of the cornea; the most common form of this condition is keratoconus. Collagen cross-linking is a non-surgical treatment intended to slow progression of corneal ectasia by strengthening corneal tissue. The standard protocol calls for application directly to the eye of a 0.1% riboflavin solution for 30 minutes followed by 30 minutes of ultraviolet-A irradiation with a wavelength of 370 nm and power of 3 mW/cm2. Under the conditions used for corneal collagen cross-linking, riboflavin 5‘-phosphate functions as a photo enhancer and generates singlet oxygen which is responsible for the cross-linking.
Primaquine is a oral medication used to treat and prevent malaria and to treat Pneumocystis pneumonia. Specifically it is used for malaria due to Plasmodium vivax and Plasmodium ovale along with other medications and for prevention if other options cannot be used. Primaquine is an alternative treatment for Pneumocystis pneumonia together with clindamycin. Primaquine is lethal to P. vivax and P. ovale in the liver stage, and also to P. vivax in the blood stage through its ability to do oxidative damage to the cell. However, the exact mechanism of action is not fully understood. Primaquine is well-absorbed in the gut and extensively distributed in the body without accumulating in red blood cells. Administration of primaquine with food or grapefruit juice increases its oral bioavailibity. In blood, about 20% of circulating primaquine is protein-bound, with preferential binding to the acute phase protein orosomucoid. With a half-life on the order of 6 hours, it is quickly metabolized by liver enzymes to carboxyprimaquine, which does not have anti-malarial activity. Common side effects of primaquine administration include nausea, vomiting, and stomach cramps. Primaquine phosphate is recommended only for the radical cure of vivax malaria, the prevention of relapse in vivax malaria, or following the termination of chloroquine phosphate suppressive therapy in an area where vivax malaria is endemic. Patients suffering from an attack of vivax malaria or having parasitized red blood cells should receive a course of chloroquine phosphate, which quickly destroys the erythrocytic parasites and terminates the paroxysm. Primaquine phosphate should be administered concurrently in order to eradicate the exoerythrocytic parasites in a dosage of 1 tablet (equivalent to 15 mg base) daily for 14 days.
Status:
US Approved OTC
Source:
21 CFR 333.310(a) acne benzoyl peroxide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Benzoyl peroxide (BPO) is an organic compound in the peroxide family. It consists of two benzoyl groups bridged by a peroxide link. It is one of the most important organic peroxides in terms of applications and the scale of its production. Benzoyl peroxide is used as an acne treatment, for bleaching hair and teeth. Adverse reactions are: dryness and urticarial reaction, contact dermatitis, application site burning, application site irritation and skin irritation.
Status:
Investigational
Source:
INN:enpiroline [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Enpiroline (WR 180,409) is an antimalarial compound. It demonstrates activity against Plasmodium falciparum both in vitro and in non-immune infected subjects. Additionally, it exerts antischistosomal activity.
Status:
Investigational
Source:
USAN:CHROMIC PHOSPHATE CR 51 [USAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Chromic Phosphate Cr-51 is a radiopharmaceutical compound that has been extensively used in nuclear medicine. When administered intraperitoneally, the particulate form of chromic phosphate is pocketed in various areas of the peritoneum, or filtered out by the first lymph nodes encountered, because of the too large particle size, whereas the colloidal form is carried over to the lymphatic system. The larger particles originally present in its size spectrum or formed in vivo by aggregation of smaller particles are trapped by the first line of lymph nodes, and the remainder goes into the thoracic duct, with posterior incorporation into the blood circulation and final removal by the reticuloendothelial system: liver, spleen and bone marrow.
Triciribine is a purine analogue which inhibits DNA and protein synthesis, it is a synthetic tricyclic nucleoside which acts as a specific inhibitor of the Akt signaling pathway. It selectively inhibits the phosphorylation and activation of Akt1, -2 and -3 but does not inhibit Akt kinase activity nor known upstream Akt activators such as PI 3-Kinase and PDK1. It inhibits cell growth and induces apoptosis preferentially in cells that express aberrant Akt1. In whole cells triciribine is phosphorylated by adenosine kinase which may be necessary for its activity. Triciribine is a cancer drug which was first synthesised in the 1970s and trialled clinically in the 1980s and 1990s without success. Following the discovery in the early 2000s that the drug would be effective against tumours with hyperactivated Akt, it is now again under consideration in a variety of cancers. As PTX-200, the drug is currently in two early stage clinical trials in breast cancer and ovarian cancer being conducted by the small molecule drug development company Prescient Therapeutics.
Status:
Investigational
Source:
INN:megalomicin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Megalomicin is a Micromonospora-produced macrolide antibiotic complex. Megalomicin A component was studied most extensively. It inhibited the ATP-dependent acidification of lysosomes and intra-Golgi transport in vitro. Megalomicin induces a powerful inhibitory effect on HIV-1 replication at nontoxic concentrations by preventing the processing of HIV-1 gp160 envelope protein and the subsequent formation of infectious viral particles.
Status:
Investigational
Source:
INN:ristianol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Ristianol (Ristianol phosphate) is a bioactive chemical that is registered as an anti-inflammatory agent and immunoregulator (in Europe), but no further information is available.
Status:
Investigational
Source:
INN:rosaramicin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Rosamaricin is a macrolide antibiotic similar to erythromycin. This compound is more effective against Gram-negative bacteria than erythromycin, especially in the prostate where rosamaricin was shown to be more concentrated than erythromycin in dogs. Rosamaricin has antibiotic activity against Neisseria gonorrhoeae, Chlamydia trachomatis, Ureaplasma urealyticum and Mycoplasma hominis. When the drug was compared with penicillin G in the treatment of pneumococcal meningitis in rabbits it was found to be less effective than penicillin G, as measured by bacterial clearance from cerebrospinal fluid and by treatment outcome. No information on the current use of this compound is available.
Status:
Investigational
Source:
INN:enazadrem [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Enazadrem (CP-70490-09) is an antipsoriatic agent inhibiting arachidonate 5-lipoxygenase.

Showing 11 - 20 of 297 results