FINERENONE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C21H22N4O3
Molecular Weight	378.4244
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCOC1=NC=C(C)C2=C1[C@H](C3=CC=C(C=C3OC)C#N)C(C(N)=O)=C(C)N2

InChI

InChIKey=BTBHLEZXCOBLCY-QGZVFWFLSA-N

InChI=1S/C21H22N4O3/c1-5-28-21-18-17(14-7-6-13(9-22)8-15(14)27-4)16(20(23)26)12(3)25-19(18)11(2)10-24-21/h6-8,10,17,25H,5H2,1-4H3,(H2,23,26)/t17-/m1/s1

HIDE SMILES / InChI

Molecular Formula	C21H22N4O3
Molecular Weight	378.4244
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/215341s000lbl.pdf

Finerenone (Kerendia®), a first-in-class, orally administered, selective, nonsteroidal mineralocorticoid receptor antagonist (MRA), is being developed by Bayer HealthCare Pharmaceuticals for the treatment of diabetic kidney disease (DKD) and heart failure (HF), including chronic HF (CHF). Finerenone blocks MR mediated sodium reabsorption and MR overactivation in both epithelial (e.g., kidney) and nonepithelial (e.g., heart, and blood vessels) tissues. MR overactivation is thought to contribute to fibrosis and inflammation. Finerenone has a high potency and selectivity for the MR and has no relevant affinity for androgen, progesterone, estrogen, and glucocorticoid receptors. Finerenone has been approved in the USA to reduce the risk of sustained estimated glomerular filtration rate (eGFR) decline, end stage renal disease (ESRD), cardiovascular death, nonfatal myocardial infarction (MI), and hospitalization for HF in adults with chronic kidney disease (CKD) associated with type 2 diabetes (T2D). Finerenone is undergoing regulatory assessment in the EU and in China. A phase III trial is investigating finerenone in patients who have HF with preserved ejection fraction.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Mineralocorticoid receptor 53 Target ID: CHEMBL1994 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24621652 \| https://www.ncbi.nlm.nih.gov/pubmed/22866979	Antagonist 2849		16.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Chronic kidney disease associated with type 2 diabetes 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/215341s000lbl.pdf	Primary		Approved 8583	Kerendia Approved Use Indicated to reduce the risk of sustained eGFR decline, end stage kidney disease, cardiovascular death, non-fatal myocardial infarction, and hospitalization for heart failure in adult patients with chronic kidney disease associated with type 2 diabetes Launch Date 2021

C_max

Value	Dose	Co-administered	Analyte	Population
80 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=30 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
160 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=30 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.431 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=146	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.54 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=146	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
25.45 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=146	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
42.49 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=147	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
63.58 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=147	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
154.4 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=147	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
90.54 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=149	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
177.3 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=149	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
287.2 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=149	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
94.54 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
170.6 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
258.6 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
167.2 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
95.5 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
105 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
110 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
88.4 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
45.9 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=164	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
47.2 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=164	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
47.6 μg/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=164	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Co-administered	Analyte	Population
343 ng × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=30 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
686 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=30 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
12.99 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=146	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
25.23 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=146	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
51.13 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=146	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
132.1 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=147	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
161.4 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=147	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
470.3 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=147	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
208.3 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=149	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
318.5 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=149	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
928.7 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=149	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
232.5 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
420.7 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1022 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
661 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
218 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
221 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
352 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
317 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
118 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=164	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
150 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=164	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
108 μg × h/L OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=164	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
2.6 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=30 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32	10 mg 1 times / day steady-state, oral dose: 10 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.6 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=30 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32	20 mg 1 times / day steady-state, oral dose: 20 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.702 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=146	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.741 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=146	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.874 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=146	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.066 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=147	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.776 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=147	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.834 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=147	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.779 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=149	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1.685 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=149	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.044 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=149	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.564 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	10 mg 2 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.832 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
3.112 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	40 mg 1 times / day multiple, oral dose: 40 mg route of administration: Oral experiment type: MULTIPLE co-administered:		FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
4.295 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=150	20 mg 2 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2.21 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.26 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.78 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=159	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2.71 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=164	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3.18 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=164	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2.29 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=164	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered: MIDAZOLAM	MIDAZOLAM	FINERENONE plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
8.3% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=31 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=89 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=128			FINERENONE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
40 mg 1 times / day multiple, oral Highest studied dose Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf
40 mg single, oral Highest studied dose Dose: 40 mg Route: oral Route: single Dose: 40 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: unknown Food Status: FASTED Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf
20 mg 1 times / day multiple, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1	Disc. AE: Adverse event, Adverse event... Other AEs: Adverse event... AEs leading to discontinuation/dose reduction: Adverse event (26%) Adverse event (2.2%) Adverse event (other than Hyperkalemia) (4.7%) Hyperkalemia (2.3%) Other AEs: Adverse event (27.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1

AEs

AE	Significance	Dose	Population
Adverse event	2.2% Disc. AE	20 mg 1 times / day multiple, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1
Hyperkalemia	2.3% Disc. AE	20 mg 1 times / day multiple, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1
Adverse event	26% Disc. AE	20 mg 1 times / day multiple, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1
Adverse event	27.2%	20 mg 1 times / day multiple, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1
Adverse event (other than Hyperkalemia)	4.7% Disc. AE	20 mg 1 times / day multiple, oral Studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf https://clinicaltrials.gov/ct2/show/NCT04795726?term=FIDELIO-&draw=2&rank=1

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inducer 1087 inhibitor 2252	inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A1 132 UGT2B7 197 CYP2C19 2057 P-gp 1741 BCRP 910 CYP1A2 2153 OCT2 779 OATP1B1 1079 OAT1 725 OATP1B3 961 OCT1 620 MATE2K 17 UGT1A1 246 CYP2B6 926 MATE1 415 CYP2C8 1057 OAT3 747 UGT1A6 136 UGT2B4 23 UGT1A4 98 UGT1A9 148	P-gp 2052 OATP1B1 503 OCT1 393 BCRP 697 OATP1B3 435 CYP1A1 389 CYP3A5 446 CYP3A7 109 CYP2C8 810	CYP1A2 832 CYP2B6 669 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=135 Page: 135 \| 136	no [IC50 >50 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=135 Page: 135 \| 136	no [IC50 >50 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=135 Page: 135 \| 136	no [IC50 >50 uM]
UGT1A1 303	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=136 Page: 136.0	no [IC50 >50 uM]
UGT1A4 100	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=136 Page: 136.0	no [IC50 >50 uM]
UGT1A6 171	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=136 Page: 136.0	no [IC50 >50 uM]
UGT1A9 155	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=136 Page: 136.0	no [IC50 >50 uM]
UGT2B4 23	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=136 Page: 136.0	no [IC50 >50 uM]
UGT2B7 210	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=136 Page: 136.0	no [IC50 >50 uM]
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=137 Page: 137.0	no
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=143 Page: 143 \| 75	no
MATE2K 17	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=143 Page: 143 \| 75	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=142 Page: 142 \| 75	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=142 Page: 142 \| 75	no
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=144 Page: 144.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=144 Page: 144 \| 75	no
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=33 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=75 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=141 Page: 33 \| 75 \|141	yes [IC50 17.4 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=33 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=134 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=171 Page: 33 \| 134 \| 170 \| 171	yes [IC50 19 uM]	no (co-administration study) Comment: Finerenone (QD, 10 days) did not effect on Midazolam (single dose) exposure (AUC and Cmax by 1.1-fold) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=33 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=134 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=171 Page: 33 \| 134 \| 170 \| 171
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=134 Page: 134 \| 135 \| 136	yes [IC50 29 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=142 Page: 142 \| 75	yes [IC50 3.2 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=134 Page: 134 \| 135 \| 136	yes [IC50 31 uM]
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=33 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=75 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=140 Page: 33 \| 75 \| 140	yes [IC50 47 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=33 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=134 Page: 33 \| 134 \| 135 \| 136	yes [IC50 6.8 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=142 Page: 142 \| 75	yes [IC50 7.6 uM]
CYP1A1 272	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=33 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=134 Page: 33 \| 134 \| 135	yes [IC50 9.5 uM]
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=137 Page: 137.0	yes
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=137 Page: 137.0	yes
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=137 Page: 137.0	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=74 Page: 32 \| 74	major	yes (co-administration study) Comment: Erythromycin increased finerenone AUC by 248% and Cmax by 88% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=74 Page: 32 \| 74
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=74 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=169 Page: 32 \| 74 \| 169	minor	yes (co-administration study) Comment: Gemfibrozil, increased finerenone AUC and Cmax by only 10.1% and 15.7%, Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=74 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=169 Page: 32 \| 74 \| 169
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=31 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=141 Page: 31 \| 141	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=31 Page: 31.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=31 Page: 31.0	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=31 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=144 Page: 31 \| 144	no
CYP1A1 389	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=130 Page: 130 \| 133	weak
CYP3A5 446	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=130	weak
CYP3A7 109	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=130 Page: 130.0	weak
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=31 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=140 Page: 31 \| 140	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/215341Orig1s000IntegratedR.pdf#page=89 Page: 89.0

PubMed

Title	Date	PubMed
Discovery of BAY 94-8862: a nonsteroidal antagonist of the mineralocorticoid receptor for the treatment of cardiorenal diseases.	2012 Aug	22791416
Mineralocorticoid receptor antagonists for the treatment of hypertension and diabetic nephropathy.	2012 Sep 27	22866979
Safety and tolerability of the novel non-steroidal mineralocorticoid receptor antagonist BAY 94-8862 in patients with chronic heart failure and mild or moderate chronic kidney disease: a randomized, double-blind trial.	2013 Aug	23713082
Renin-angiotensin system blockade: Finerenone.	2017 Apr	28577743

Patents

Sample Use Guides

In Vivo Use Guide

The recommended starting dosage is 10 mg or 20 mg orally once daily based on estimated glomerular filtration rate (eGFR) and serum potassium thresholds. (2.1) • Increase dosage after 4 weeks to the target dose of 20 mg once daily, based on eGFR and serum potassium thresholds. (2.3) • Tablets may be taken with or without food

Route of Administration: Oral

In Vitro Use Guide

Finerenone had an IC50 of 17 nM in the MR, but no activity up to 10 uM in the other steroid hormone receptors.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 21:32:05 GMT 2025` Edited by `admin` on `Mon Mar 31 21:32:05 GMT 2025`
Record UNII	DE2O63YV8R
Record Status	`Validated (UNII)`
Record Version

Download

Name

Type

Language

BAY 94-8862

Preferred Name

English

FINERENONE

Official Name

English

finerenone [INN]

Common Name

English

1,6-NAPHTHYRIDINE-3-CARBOXAMIDE, 4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-1,4-DIHYDRO-2,8-DIMETHYL-, (4S)-

Systematic Name

English

FINERENONE [ORANGE BOOK]

Common Name

English

FINERENONE [USAN]

Common Name

English

KERENDIA

Brand Name

English

FINERENONE [JAN]

Common Name

English

Finerenone [WHO-DD]

Common Name

English

BAY-94-8862

Code

English

(4S)-4-(4-Cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide

Systematic Name

English

Code System Code Type Description

EPA CompTox

DTXSID10146928