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Status:
US Approved Rx
(2017)
Source:
ANDA207092
(2017)
Source URL:
First approved in 2001
Source:
CANCIDAS by MERCK
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Caspofungin is an echinocandin antifungal drug, which is approved and is sold under the brand worldwide name cancidas. Caspofungin inhibits the synthesis of beta (1,3)-D-glucan, an essential component of the cell wall of susceptible Aspergillus species and Candida species. Beta (1,3)-D-glucan is not present in mammalian cells. Cancidas is indicated for the treatment of candidemia and the following candida infections: intra-abdominal abscesses, peritonitis, and pleural space infections in adult and pediatric patients. Also is indicated for the treatment of esophageal candidiasis in adult and pediatric patients and for the treatment of invasive aspergillosis in adult and pediatric patients, but has not been studied as initial therapy for invasive aspergillosis.
Status:
US Approved Rx
(2010)
Source:
ANDA065238
(2010)
Source URL:
First approved in 1978
Source:
MEFOXIN by NORVIUM BIOSCIENCE
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Cefoxitin is a cephamycin antibiotic often grouped with the second-generation cephalosporins. It is active against a broad range of gram-negative bacteria including anaerobes. The methoxy group in the 7a position provides cefoxitin with a high degree of stability in the presence of beta-lactamases, both penicillinases and cephalosporinases, of gram-negative bacteria. The bactericidal action of cefoxitin results from inhibition of cell wall synthesis.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
JANEX-1 (WHI-P131), a selective Janus kinase 3 (JAK3) inhibitor, has been shown to delay the onset of diabetes in the NOD mouse model. It is a cell-permeable, reversible, potent, ATP-competitive, and specific inhibitor of JAK3 (IC50 = 78 uM); has no effect on JAK1, JAK2, or Zap/Syk or SRC tyrosine kinases. JANEX-1 has a potent inhibitory effect on cytokine-induced β-cell damage. JANEX-1 has a therapeutic potential in the treatment and prevention of type 1 diabetes. JANEX-1 induced apoptosis in JAK3-expressing human leukemia cell lines NALM-6 and LC1. JANEX-1 inhibited the clonogenic growth of JAK3-positive leukemia cell lines DAUDI, RAMOS, LC1;19, NALM-6, MOLT-3, and HL-60 (but not JAK3-negative BT-20 breast cancer, M24-MET melanoma, or SQ20B squamous carcinoma cell lines) in a concentration-dependent fashion. Potent and specific inhibitors of JAK3 such as JANEX-1 may provide the basis for the design of new treatment strategies against acute lymphoblastic leukemia, the most common form of childhood cancer. JANEX-1/WHI-P131 also showed potent anti-inflammatory activity in several cellular and in vivo animal models of inflammation, including mouse models of peritonitis, colitis, cellulitis, sunburn, and airway inflammation with favorable toxicity and pharmacokinetic profile. JANEX-1 may prove useful to prevent or alleviate the symptoms of endometriosis (EMS).
Status:
Other
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
A-987306 is a new histamine H(4) antagonist. A-987306 is potent in H(4) receptor binding assays (rat H(4), K(i) = 3.4 nM, human H(4) K(i) = 5.8 nM) and demonstrated potent functional antagonism in vitro at human, rat, and mouse H(4) receptors in cell-based FLIPR assays. A-987306 also demonstrated H(4) antagonism in vivo in mice, blocking H(4)-agonist induced scratch responses, and showed anti-inflammatory activity in mice in a peritonitis model. Most interesting was the high potency and efficacy of this compound in blocking pain responses, where it showed an ED(50) of 42 umol/kg (ip) in a rat post-carrageenan thermal hyperalgesia model of inflammatory pain. A-987306 inhibited the scratching response (IC50 = 0.4 umoles/kg, i.p.) with (85%) inhibition seen at 30 umoles/kg, i.p. A-987306 is a potent and selective H4R antagonist with robust antipruritic activity and is a useful tool for further exploration of the role of H4R receptors in vivo.
Status:
Other
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
A-943931 is a potent and selective H4R antagonist with high affinity at both human (Kis = 4.6 nM) and rat (Kis = 3.8 nM) receptors. A-943931 competitively and potently antagonizes rat H4R agonist-mediated responses in [35S]GTPγS binding assays (Kbs = 28 nM) and intracellular calcium mobilization at rat and human receptors (Kbs from 5-10 nM). When tested in vivo in a mouse model of clobenpropit (10 nM, i.d.) induced scratching, A-943931 inhibited the scratching response (IC50 = 26 umoles/kg, i.p.) with significant inhibition (69%) at the highest tested dose (30 umoles/kg, i.p.). A-943931 is a potent and selective H4R antagonist with robust antipruritic activity and is a useful tool for further exploration of the role of H4R receptors in vivo.
Status:
Other
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
IMB-10 stabilizes binding of alpha(M)beta(2) to its endogenous ligands proMMP-9 and fibrinogen. It inhibited alpha(M)beta(2)-dependent migration in vitro and inflammation-induced neutrophil emigration in vivo. IMB-10 therapy inhibited the growth of both leukemia and lymphoma xenografts and significantly prolonged the survival of the mice with lymphoma. IMB-10 has potential as a therapy for leukocytic malignancies, particularly for lymphomas.
Cresopirine is benzoic acid derivative and o-Cresotic Acid ester with anti-inflammatory activity.
Status:
US Previously Marketed
Source:
MANDOL by LILLY
(1978)
Source URL:
First approved in 1978
Source:
MANDOL by LILLY
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cefamandole (also known as cephamandole) is a broad-spectrum cephalosporin antibiotic. The clinically used form of cefamandole is an ester form, cefamandole nafate, a prodrug. Cefamandole is no longer available in USA, but it has prescription in UK. Cefamandole under brand name mandol is indicated for the treatment of serious infections caused by susceptible strains of the designated microorganisms such as: lower respiratory infections, including pneumonia, caused by S. pneumoniae. So as urinary tract infections caused by E. coli, Proteus spp.; peritonitis caused by E. coli and Enterobacter spp. Septicemia caused by E. coli; skin and skin structure infections caused by S. aureus; bone and joint infections caused by S. aureus (penicillinase- and non-penicillinase-producing). Like all beta-lactam antibiotics, cefamandole binds to specific penicillin-binding proteins (PBPs) located inside the bacterial cell wall, causing the inhibition of the third and last stage of bacterial cell wall synthesis. Bacterial cell wall autolytic enzymes such as autolysins then mediate cell lysis; it is possible that cefamandole interferes with an autolysin inhibitor.
Status:
Possibly Marketed Outside US
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Noxythiolin is an antimicrobial agent. It can be used for irrigation procedures with noxythiolin solution to reduce the risk of sepsis in patients undergoing percutaneous drainage procedures. It seems mechanism of action is based on ability of noxythiolin to decompose in solution to liberate most of its formaldehyde.
Status:
Possibly Marketed Outside US
Source:
Ceftezole sodium for injection by Fujisawa Pharmaceutical
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ceftezole sodium is a cephalosporin antibiotic. Ceftezole was found to be a broad-spectrum antibiotic, active in vitro against many species of gram-positive and gram-negative bacteria except Pseudomonas aeruginosa, Serratia marcescens and Proteus vulgaris. Ceftezole sodium is used as an injectable or through an intravenous mode of delivery. The bactericidal activity of ceftezole results from the inhibition of cell wall synthesis via affinity for penicillin-binding proteins (PBPs). The PBPs are transpeptidases which are vital in peptidoglycan biosynthesis. Therefore, their inhibition prevents this vital cell wall component from being properly synthesized. Ceftezole has been shown to exhibit potent alpha-glucosidase inhibitory activity. In in vitro alpha-glucosidase assays, ceftezole was shown to be a reversible, non-competitive inhibitor of yeast alpha-glucosidase with a Ki value of 5.78 x 10(-7) M when the enzyme mixture was pretreated with ceftezole. Ceftezole is used for the treatment of susceptible bacterial infections including septicemia, respiratory, biliary or GU tract, skin and skin structure, endocarditis. Surgical prophylaxis.