Other substances

Raloxifene

A selective benzothiophene estrogen receptor modulator.

Phase of research

Potential treatment - pre-clinical evidence

How it helps

Antiviral

Drug status

Used to treat other disease

Supporting references

Contradictory references

AI-suggested references

Clinical trials

General information

Raloxifene is a selective benzothiophene oestrogen receptor modulator. In different tissues it acts either as an agonist or as an antagonist of oestrogen receptors (NCIt).

Raloxifene on DrugBank
Raloxifene on PubChem
Raloxifene on Wikipedia

Marketed as

EVISTA; KEOXIFENE; OPTRUMA

C1CCN(CC1)CCOC2=CC=C(C=C2)C(=O)C3=C(SC4=C3C=CC(=C4)O)C5=CC=C(C=C5)O.Cl

Supporting references

Link	Tested on	Impact factor	Notes	Publication date
Identification of Potent and Safe Antiviral Therapeutic Candidates Against SARS-CoV-2 Small molecule In vitro Screening	Vero cells	5.09		Nov/25/2020
Molecular Features of Non-Selective Small Molecule Antagonists of the Bradykinin Receptors Small molecule In silico	in silico	4.29	Predicted to non-selectively bind bradykinin receptors, which was theorised to alleviate SARS-CoV-2-related inflammation.	Sep/21/2020
Heparan sulfate assists SARS-CoV-2 in cell entry and can be targeted by approved drugs in vitro Polysaccharide Small molecule In vitro	ACE2-GFP HEK293T cells; Calu-3 cells; Vero E6 cells; SARS-CoV-2 pseudotyped particles	6.26	Raloxifene treatment combined with tilorone synergistically inhibited SARS-CoV-2 pseudovirus infection in Vero E6 cells. Treatment with raloxifene alone resulted in modest virus-related cytopathic effect reduction.	Nov/04/2020

AI-suggested references

Link	Publication date
Characterization of raloxifene as a potential pharmacological agent against SARS-CoV-2 and its variants.	May/25/2022
Binding of raloxifene to human complement fragment 5a (hC5a): a perspective on cytokine storm and COVID19	Oct/20/2021
iPSC screening for drug repurposing identifies anti-RNA virus agents modulating host cell susceptibility	Feb/18/2021
Repurposing the estrogen receptor modulator raloxifene to treat SARS-CoV-2 infection	Dec/20/2021
Discovery of a Bradykinin B2 Partial Agonist Profile of Raloxifene in a Drug Repurposing Campaign	Oct/18/2021
Raloxifene as a treatment option for viral infections	Sep/28/2020
A phase 2 randomized, double-blinded, placebo-controlled, multicenter trial evaluating the efficacy and safety of raloxifene for patients with mild to moderate COVID-19.	May/12/2022
Mechanism of Caspase-1 Inhibition by Four Anti-inflammatory Drugs Used in COVID-19 Treatment	Jun/15/2021
Raloxifene and Bazedoxifene Could Be Promising Candidates for Preventing the COVID-19 Related Cytokine Storm, ARDS and Mortality.	Sep/03/2020
Repurposing existing drugs: identification of SARS-CoV-2 3C-like protease inhibitors	Jan/13/2021

Clinical trials

ID	Title	Status	Phase	Start date	Completion date
NCT05172050	Multicenter Double Blind, Parallel-group Phase 2/3 Trial, to Study Raloxifene in Adult COVID-19 Patients.	Completed	Phase 2\|Phase 3	Jan/22/2021	Jun/12/2021
Alternative id - RLX0120\|2020-003936-25 Interventions - Drug: Raloxifene\|Other: Placebo Study type - Interventional Study results - No Results Available Locations - CHU Amiens, Amiens, France\|Clinique de l'infirmerie protestante de Lyon, Caluire-et-Cuire, France\|CH Emile Roux le Puy en Velay, Le Puy-en-Velay, France\|Centre Hospitalier de Troyes, Troyes, France\|Humanitas Gavazzeni, Bergamo, Italy\|Ospedale San Salvatore, L'Aquila, Italy\|AO dei Colli (Ospedale Monaldi), Napoli, Italy\|INMI Lazzaro Spallanzani, Roma, Italy\|Istituto Clinico Humanitas, Rozzano, Italy\|A.O.U. Città della Salute e della Scienza, Torino, Italy\|Hospital Universitario Virgen de la Victoria, Málaga, Spain Study designs - Allocation: Randomized\|Intervention Model: Parallel Assignment\|Masking: Double (Participant, Investigator)\|Primary Purpose: Treatment Enrollment - 68 Age - 40 Years and older (Adult, Older Adult) Outcome measures - Proportion of participants with undetectable SARS-CoV-2 at PCR randomization\|Proportion of participants not requiring oxygen therapy and/or mechanical ventilation\|Proportion of participants with undetectable SARS-CoV-2 at PCR\|Proportion of patients in each National Early Warning Score (NEWS) category\|Mean value of National Early Warning Score (NEWS) category\|Proportion of participants with any adverse event with grade ≤ 2 after randomization.\|Proportion of participants with any severe adverse events (grade ≥ 3 according to CTCAE) after randomization\|Proportion of hospitalized participants who at the beginning of the study were at domicile isolation after randomization.\|Proportion of participants admitted to intensive care after randomization.\|Proportion of survivors\|Mean change from baseline to day 7, 14, 21 and 28 after randomization of value for biomarker parameters\|Quality of life questionnaire

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