The ChEMBL-og

ATC Code: D01AC   (incomplete) Wikipedia:  Not Available ChEMBL:  CHEMBL2105689 On November 14th the  FDA approved  Luliconazole (trade name Luzu  TM ) for the treatment of skin fungal infections including ringworm. Luliconazole inhibits fungal synthesis of ergosterol, required for fungal cell membranes, by inhibiting the enzyme cytochrome P450 14-alpha-demethylase (P45014DM) .   Target(s) Like all azole antifungals, Luliconazole binds and inhibits fungal 14-alpha-demethylase (e.g. CHEMBL1681624 , Uniprot Q96W81 ).  P45014DM is a cytochrome P450 that catalyses the oxidative removal of the 14α-methyl group from eburicol to ergosterol. Azoles bind to the haem in P45014DM  via the unprotonated N atom and occupy the active site as non-competitive inhibitors. Luliconazole ( CHEMBL2105689 ;  Pubchem :  144206495  ) is a small molecule drug with a molecular weight of 35...

ATC Code: R03AK10 Wikipedia: Vilanterol On May 10 th , the FDA approved Vilanterol (Tradename: Breo Ellipta ; Research Code: GW-642444M), a long-acting beta 2 -adrenergic agonist , in combination with the already approved fluticasone furoate , an inhaled corticosteroid , for the long-term maintenance treatment of bronchospasm associated with chronic obstructive pulmonary disease (COPD). Chronic obstructive pulmonary disease (COPD) is characterised by the occurrence of chronic bronchitis or emphysema , a pair of commonly co-existing diseases of the lungs in which the airways become narrowed. Bronchial spasms, a sudden constriction of the muscles in the walls of the bronchioles , occur frequently in COPD. Vilanterol is a new long-acting beta 2  receptor agonist that through the activation of the beta 2 adrenergic receptors present in the bronchial smooth muscle, leads to bronchodilation, and consequently eases the symptoms of COPD. The beta 2 adrenergeic re...

ATC code: not yet assigned Wikipedia: Crofelemer On December 31 2012, the FDA approved Crofelemer for the treatment of diarrhea caused by antiretroviral medication regimens taken by patients with HIV/AIDS . Diarrhea is a frequent adverse effect of antiretroviral medication - however, it can also be caused by secondary infections of the gastrointestinal tract or the virus itself. The loss of fluids incurred by diarrhea can lead to dehydration and electrolyte imbalance. As a side-effect of antiretroviral medication it also reduces patient compliance with a prescribed medication regimen. Crofelemer alleviates the symptoms of HIV-associated diarrhea by limiting the amount of chloride ions that are pumped into the intestinal lumen, thus also retaining sodium ions and water. Crofelemer is a natural product oligomer that is not orally bioavailable but acts locally on the intestinal surface. It was shown to inhibit two distinct intestinal chloride channels expressed in...

On Jan 23rd 2012 the FDA approved Ingenol mebutate gel for the topical treatment of actinic keratosis (AK). Ingenol mebutate (trade name: PICATO ®, formally known as PEP-005) is a natural product derived from the euphorbia plant. Actinic, or solar keratosis ( Wikipedia ; NIH ; OMIM ) is a pre-cancerous pigmented lesion on the skin, most commonly occurring in skin that has been frequently exposed to the sun. If left untreated, about 20% of cases transform into Squamous Cell Carcinoma . Ingenol mebutate induces cell death in Actinic Keratosis. The precise targets responsible for the mechanism of action is not known, however, Ingenol derivatives (see e.g. CHEMBL346507 ) have been shown to have anticancer activities. Many of these derivatives have activity on several Protein Kinase C isoforms. Mechanistically Ingenol mebutate causes rapid lesion necrosis and also specific neutrophil-mediated, antibody-dependent cellular cytotoxicity Ingenol mebutate (IUPAC: 2-Butenoic acid, ...