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Dutasteride (Avodart) was the second steroidal 5α-reductase approved after finasteride. It is a competitive inhibitor of all three 5α-reductase isoenzymes [ 4 ] and it inhibits types 1 and 2 better than finasteride, leading to it causing further reduction in DHT, with >90% reduced DHT levels following 1 year of oral administration.
Rivaroxaban (Xarelto) was the first approved FXa inhibitor to become commercially available in Europe and Canada in 2008. [1] The second one was apixaban (Eliquis), approved in Europe in 2011 [2] and in the United States in 2012. [3] The third one edoxaban (Lixiana, Savaysa) was approved in Japan in 2011 and in Europe and the US in 2015. [4]
Abacavir was approved by the FDA for use in therapy of HIV-1 infections in December 1998. [20] This drug is the only approved antiretroviral that is active as a guanosine analogue in vivo. First it is monophosphorylated by adenosine phosphotransferase and then the monophosphate is converted to carbovir 3´-monophosphate.
Eliglustat, sold under the brand name Cerdelga, is a medication used for the treatment of Gaucher's disease. It was discovered at the University of Michigan, developed by Genzyme Corp, and was approved by the FDA in August 2014. [7] Commonly used as the tartrate salt, the compound is believed to work by inhibition of glucosylceramide synthase.
The discovery of T-1095 led to an investigation [when?] of how to enhance potency, selectivity and oral bioavailability by adding various substituents to the glycoside core. As an example we can take the change of o-glycosides to c-glycosides by creating a carbon–carbon bond between the glucose and the aglycone moiety.
It was approved by the Food and Drug Administration (FDA) in 1998 as the first oral medicine for erectile dysfunction. Later, in the year 2005, it was approved for the treatment of pulmonary arterial hypertension. [2] Vardenafil and tadalafil were discovered in 1990.
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