Raloxifene - Existing Drug with Potential for Treating COVID-19

Raloxifene - Existing Drug with Potential for Treating COVID-19

Posted by Valerie Walters on Jul 13, 2020 3:03 am

A private-public consortium funded by the EXSCALATE4CoV project has announced promising results for the fight against the coronavirus. According to the announcement, “an already registered generic drug used to treat osteoporosis, Raloxifene, could be an effective treatment for COVID-19 patients with mildly symptomatic infection,” as stated by the European Commission. 7 000 molecules were preselected and further tested ‘in vitro’. Raloxifene emerged as a promising molecule: according to the project, it could be effective in blocking the replication of the virus in cells and could thus hold up the progression of the disease.

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Raloxifene (CAS No.: 84449-90-1) is a member of the class of 1-benzothiophenes that is 1-benzothiophene in which the hydrogens at positions 2, 3, and 6 have been replaced by p-hydroxyphenyl, p-[2-(piperidin-1-yl)ethoxy]benzoyl, and hydroxy groups, respectively. It has a role as a bone density conservation agent, an estrogen receptor modulator, and an estrogen antagonist. It is a member of phenols, an aromatic ketone, a member of 1-benzothiophenes, and an N-oxyethylpiperidine. It is a conjugate base of raloxifene(1+).

Raloxifene is a selective estrogen receptor modulator that partially mimics the effects of estrogens in bone and the cardiovascular system and has estrogen antagonist properties in endometrial and breast tissue.
Mechanism of Action: Raloxifene appears to influence gene transcription, via the intermediary of estrogen receptors (ER), through interactions with the estrogen response element (ERE) and a distinct DNA target, the raloxifene response element (RRE). However, the precise mechanism of action of this agent remains to be elucidated.

Bone Remodelling: Raloxifene modulates bone cell homeostasis in vitro, through actions on the proliferation and activity of osteoclasts and osteoblasts. Effects include inhibition of osteoclast pit formation and increases in the expression of bone matrix proteins such as alkaline phosphatase, osteonectin, osteocalcin, and collagen.

List of raloxifene and related compounds:
Raloxifene
Raloxifene Hydrochloride
Trioxifene
Pitofenone

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