molidustat

Small moleculeexperimental

Molidustat is a drug which acts as an HIF prolyl-hydroxylase inhibitor and thereby increases endogenous production of erythropoietin, which stimulates production of hemoglobin and red blood cells. It is in Phase III clinical trials for the treatment of anemia caused by chronic kidney disease. Due to its potential applications in athletic doping, it has also been incorporated into screens for performance-enhancing drugs. — Wikipedia

Clinical trial activity

15 trials · 1 clinical orgs · 0 marketing orgs

Phase 1

Phase 2

Phase 3

Phase 4

Earliest trial started Mar 1, 2011 (NCT01318551)

Timeline

2010s

Jan 1, 2011
Earliest Phase 1 Sponsor(trial)
Jan 1, 2013
Earliest Phase 2 Sponsor(trial)
Jan 1, 2017
Earliest Phase 3 Sponsor(trial)

Indications

Studied for

Mechanism of action

Hypoxia inducible factors; HIF-1-alpha, HIF-2-alphaINHIBITOR
Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha inhibitor
- Hypoxia-inducible factor 1-alpha (HIF1A) ↗
- Endothelial PAS domain-containing protein 1 (EPAS1) ↗
- Hypoxia-inducible factor 1 alpha
- Endothelial PAS domain-containing protein 1
Hypoxia-inducible factor prolyl hydroxylase 1INHIBITOR
Hypoxia-inducible factor prolyl hydroxylase 1 inhibitor
May exert its effect on renal anemia by increasing Hb via activation of the HIF pathway. Active against PHD1-3 but activity against PHD2 may be the most significant for the therapeutic effect.
Active against PHD1-3 but activity against PHD2 may be the most significant for the therapeutic effect.
- Egl nine homolog 2 (EGLN2) ↗
Egl nine homolog 3INHIBITOR
Egl nine homolog 3 inhibitor
May exert its effect on renal anemia by increasing Hb via activation of the HIF pathway. Active against PHD1-3 but activity against PHD2 may be the most significant for the therapeutic effect.
Active against PHD1-3 but activity against PHD2 may be the most significant for the therapeutic effect.
- Egl nine homolog 3 (EGLN3) ↗
Egl nine homolog 1INHIBITOR
Egl nine homolog 1 inhibitor
May exert its effect on renal anemia by increasing Hb via activation of the HIF pathway. Active against PHD1-3 but activity against PHD2 may be the most significant for the therapeutic effect.
Active against PHD1-3 but activity against PHD2 may be the most significant for the therapeutic effect.
- Egl nine homolog 1 (EGLN1) ↗

Chemistry & pharmacology

Loading structure…

SMILES

O=c1c(-n2ccnn2)c[nH]n1-c1cc(N2CCOCC2)ncn1

Mol. weight: 314.31 g/mol
Lipinski Ro5: Pass
Rule of 3: No
Chirality: Achiral Molecule
Inorganic: No
Polymer: No

Oral

Parenteral

Topical

Sources

WikipediaMolidustat ↗
ChEMBLCHEMBL3646118 ↗

Also known as

2-(6-(morpholin-4-yl)pyrimidin-4-yl)-4-(1h-1,2,3-triazol-1-yl)-1,2-dihydro-3h-pyrazol-3-one
bay 85-3934
bay85-3934
bay85-3934
molidustat
molidustat
molidustat

Clinical trials

NCT ID	Phase	Start date	Sponsor(s)
NCT03543657	Phase 3	Jun 23, 2018	Bayer
NCT03418168	Phase 3	Feb 22, 2018	Bayer
NCT03351166	Phase 3	Jan 22, 2018	Bayer
NCT03350347	Phase 3	Dec 13, 2017	Bayer
NCT03350321	Phase 3	Dec 12, 2017	Bayer
NCT02312973	Phase 1	Jan 1, 2015	Bayer
NCT02055482	Phase 2	Jun 1, 2014	Bayer
NCT02064426	Phase 2	Mar 1, 2014	Bayer
NCT02021370	Phase 2	Feb 1, 2014	Bayer
NCT02021409	Phase 2	Jan 1, 2014	Bayer
NCT01975818	Phase 2	Oct 1, 2013	Bayer
NCT01679587	Phase 1	Sep 1, 2012	Bayer
NCT01458028	Phase 1	Sep 1, 2011	Bayer
NCT01332942	Phase 1	Apr 1, 2011	Bayer
NCT01318551	Phase 1	Mar 1, 2011	Bayer

Showing 15 of 15 trials

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Organizations

Research & Development (1)

Organization	Org type	Trials	As lead sponsor	Phases	Earliest year
Bayer	For profit	15	15	3	2011

1 organizations

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