HIF Prolyl-hydroxylase Inhibitor
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Not to be confused with '' Factor Inhibiting HIF Asparaginyl Hydroxylase Inhibitors'' Hypoxia-inducible factor prolyl hydroxylase Inhibitors (HIF-PHIs) also known as hypoxia-inducible factor stabilizers (HIF stabilizers) are members of a mostly experimental class of drugs that act by inhibiting
hypoxia-inducible factor-proline dioxygenase Hypoxia-inducible factor-proline dioxygenase (, ''HIF hydroxylase'') is an enzyme with systematic name ''hypoxia-inducible factor-L-proline, 2-oxoglutarate:oxygen oxidoreductase (4-hydroxylating)''. This enzyme catalyses the following chemical rea ...
(HIF prolyl-hydroxylase) which is responsible to break down the
hypoxia-inducible factor Hypoxia-inducible factors (HIFs) are transcription factors that respond to decreases in available oxygen in the cellular environment, or hypoxia. They are only present in parahoxozoan animals. Discovery The HIF transcriptional complex wa ...
(HIF) under conditions of normal oxygen concentrations. they had been investigated in in cell models for the treatment of
anemia Anemia or anaemia (British English) is a blood disorder in which the blood has a reduced ability to carry oxygen due to a lower than normal number of red blood cells, or a reduction in the amount of hemoglobin. When anemia comes on slowly, th ...
,
chronic kidney disease Chronic kidney disease (CKD) is a type of kidney disease in which a gradual loss of kidney function occurs over a period of months to years. Initially generally no symptoms are seen, but later symptoms may include leg swelling, feeling tired, vo ...
(CKD),
ischemia Ischemia or ischaemia is a restriction in blood supply to any tissue, muscle group, or organ of the body, causing a shortage of oxygen that is needed for cellular metabolism (to keep tissue alive). Ischemia is generally caused by problems wi ...
including ischemia of the heart tissue, cancer, and others. Research conducted in mice suggests that they may increase
hippocampal The hippocampus (via Latin from Greek , 'seahorse') is a major component of the brain of humans and other vertebrates. Humans and other mammals have two hippocampi, one in each side of the brain. The hippocampus is part of the limbic system, an ...
memory by increasing
erythropoietin Erythropoietin (; EPO), also known as erythropoetin, haematopoietin, or haemopoietin, is a glycoprotein cytokine secreted mainly by the kidneys in response to cellular hypoxia; it stimulates red blood cell production (erythropoiesis) in the bo ...
expression. research focuses mainly on anemia associated with CKD, and to some extent on ischemia. One drug of this class (
roxadustat Roxadustat, sold under the brand name Evrenzo, is an anti-anemia medication. Roxadustat is a HIF prolyl-hydroxylase inhibitor that increases endogenous production of erythropoietin and stimulates production of hemoglobin and red blood cells. It ...
) is marketed in China and Japan for the treatment of anaemia in CKD patients.


Examples

*
Daprodustat Daprodustat, sold under the brand name Duvroq among others, is a medication that is used for the treatment of anemia due to chronic kidney disease. It is a hypoxia-inducible factor prolyl hydroxylase inhibitor. It is taken by mouth. The most ...
* Desidustat * Enarodustat * Molidustat *
Roxadustat Roxadustat, sold under the brand name Evrenzo, is an anti-anemia medication. Roxadustat is a HIF prolyl-hydroxylase inhibitor that increases endogenous production of erythropoietin and stimulates production of hemoglobin and red blood cells. It ...
(marketed in China) *
Vadadustat Vadadustat, sold under the brand name Vafseo is a medication used for the treatment of symptomatic anemia associated with chronic kidney disease. Text was copied from this source which is copyright European Medicines Agency. Reproduction is au ...


See also

* Hypoxia-inducible factors#As a therapeutic target


References

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