ROXADUSTAT

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H16N2O5
Molecular Weight	352.3407
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=NC(C(=O)NCC(O)=O)=C(O)C2=C1C=C(OC3=CC=CC=C3)C=C2

InChI

InChIKey=YOZBGTLTNGAVFU-UHFFFAOYSA-N

InChI=1S/C19H16N2O5/c1-11-15-9-13(26-12-5-3-2-4-6-12)7-8-14(15)18(24)17(21-11)19(25)20-10-16(22)23/h2-9,24H,10H2,1H3,(H,20,25)(H,22,23)

HIDE SMILES / InChI

Molecular Formula	C19H16N2O5
Molecular Weight	352.3407
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://newdrugapprovals.org/2016/06/21/roxadustat/
Curator's Comment: Description was created based on several sources, including https://www.sps.nhs.uk/medicines/roxadustat/ http://adisinsight.springer.com/drugs/800023523

Roxadustat (FG-4592) is an HIF α prolyl hydroxylase inhibitor in a cell-free assay. It stabilizes HIF-2 and induces EPO production and stimulates erythropoiesis. Roxadustat transiently and moderately increased endogenous erythropoietin and reduced hepcidin. It is currently being investigated as an oral treatment for anemia associated with chronic kidney disease (CKD). In April 2006, Roxadustat (FG-4592) was licensed to Astellas Pharma by originator FibroGen in Asia, Europe and South Africa for the treatment of anemia. FibroGen retains rights in the rest of the world. In 2007, the FDA put the trial on clinical hold due to one case of death by fulminant hepatitis during a phase II clinical trial for patients with anemia associated with chronic kidney disease and not requiring dialysis. However, in 2008, the FDA informed the company that clinical trials could be resumed. Phase II/III clinical trials for this indication resumed in 2012. In 2013, the compound was licensed to AstraZeneca by FibroGen for development and marketing in US, CN and all major markets excluding JP, Europe, the Commonwealth of Independent States, the Middle East and South Africa, for the treatment of anemia associated with chronic kidney disease (CKD) and end-stage renal disease (ESRD).

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Hypoxia-inducible factor prolyl hydroxylase 1 6 Target ID: CHEMBL3028 Sources: https://www.ncbi.nlm.nih.gov/pubmed/27352308	Inhibitor 8504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Anemia 70 Sources: https://clinicaltrials.gov/ct2/show/NCT02174627	Primary		Phase III 665	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
6975 ng/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/27352308/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=71	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8498 ng/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/27352308/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=71	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
6780 ng/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6730 ng/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6910 ng/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6950 ng/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
10.4 μg/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/29966038/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K102_1.pdf#page=11	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.82 μg/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/29966038/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K102_1.pdf#page=11	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
8.41 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29981285/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1.9 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	0.3 mg/kg bw single, oral dose: 0.3 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.4 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	1 mg/kg bw single, oral dose: 1 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.9 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	2 mg/kg bw single, oral dose: 2 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.9 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	3 mg/kg bw single, oral dose: 3 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
20.8 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	4 mg/kg bw single, oral dose: 4 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.6 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	0.3 mg/kg bw 3 times / week multiple, oral dose: 0.3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.8 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	0.3 mg/kg bw 3 times / week multiple, oral dose: 0.3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.4 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	1 mg/kg bw 3 times / week multiple, oral dose: 1 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.2 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	1 mg/kg bw 3 times / week multiple, oral dose: 1 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.8 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	3 mg/kg bw 3 times / week multiple, oral dose: 3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.1 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	3 mg/kg bw 3 times / week multiple, oral dose: 3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
16 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29 \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K102_1.pdf#page=115	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.6 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	1 mg/kg bw single, oral dose: 1 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.4 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	1 mg/kg bw single, oral dose: 1 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
13 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	2 mg/kg bw single, oral dose: 2 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9.4 μg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	2 mg/kg bw single, oral dose: 2 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
63693 ng × h/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/27352308/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=71	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
49807 ng × h/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/27352308/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=71	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
39800 ng × h/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
82500 ng × h/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
76600 ng × h/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
77400 ng × h/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
87.5 μg × h/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/29966038/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K102_1.pdf#page=11	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
88.1 μg × h/mL OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/29966038/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K102_1.pdf#page=11	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
74.9 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29981285/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
13.8 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	0.3 mg/kg bw single, oral dose: 0.3 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
43.6 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	1 mg/kg bw single, oral dose: 1 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
99.7 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	2 mg/kg bw single, oral dose: 2 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
139.3 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	3 mg/kg bw single, oral dose: 3 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
168.8 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	4 mg/kg bw single, oral dose: 4 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.7 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	0.3 mg/kg bw 3 times / week multiple, oral dose: 0.3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	0.3 mg/kg bw 3 times / week multiple, oral dose: 0.3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
37.4 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	1 mg/kg bw 3 times / week multiple, oral dose: 1 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
39.7 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	1 mg/kg bw 3 times / week multiple, oral dose: 1 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
138.5 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	3 mg/kg bw 3 times / week multiple, oral dose: 3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
153.1 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	3 mg/kg bw 3 times / week multiple, oral dose: 3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
108.7 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29 \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K102_1.pdf#page=115	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
65.6 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	1 mg/kg bw single, oral dose: 1 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
56.6 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	1 mg/kg bw single, oral dose: 1 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
149.9 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	2 mg/kg bw single, oral dose: 2 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
135.3 μg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	2 mg/kg bw single, oral dose: 2 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
14.7 h OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/27352308/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=71	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
12.6 h OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/27352308/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=71	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
16 h OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
18.5 h OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.8 h OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
17.2 h OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
12.3 h OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/29966038/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K102_1.pdf#page=11	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.5 h OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/29966038/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K102_1.pdf#page=11	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
11.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29981285/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
8.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	0.3 mg/kg bw single, oral dose: 0.3 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	1 mg/kg bw single, oral dose: 1 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.3 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	2 mg/kg bw single, oral dose: 2 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	3 mg/kg bw single, oral dose: 3 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	4 mg/kg bw single, oral dose: 4 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	0.3 mg/kg bw 3 times / week multiple, oral dose: 0.3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	0.3 mg/kg bw 3 times / week multiple, oral dose: 0.3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.6 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	1 mg/kg bw 3 times / week multiple, oral dose: 1 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	1 mg/kg bw 3 times / week multiple, oral dose: 1 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	3 mg/kg bw 3 times / week multiple, oral dose: 3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.7 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=28	3 mg/kg bw 3 times / week multiple, oral dose: 3 mg/kg bw route of administration: Oral experiment type: MULTIPLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
17.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29 \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K102_1.pdf#page=115	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
15.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	1 mg/kg bw single, oral dose: 1 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
15.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	1 mg/kg bw single, oral dose: 1 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
20.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	2 mg/kg bw single, oral dose: 2 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
16.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=29	2 mg/kg bw single, oral dose: 2 mg/kg bw route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Analyte	Population
1.1% OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/27352308/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=71	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.81% OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/27352308/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=71	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
0.871% OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.06% OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.16% OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.1% OTHER GOV'T https://pubmed.ncbi.nlm.nih.gov/26947173/ \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K103_1.pdf#page=36	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	ROXADUSTAT plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1% OTHER GOV'T https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_A100_1.pdf#page=25 \| https://www.pmda.go.jp/drugs/2019/P20191007001/800126000_30100AMX00239_K100_1.pdf#page=156		ROXADUSTAT plasma	Homo sapiens

Doses

Dose	Population	Adverse events
5 mg/kg single, oral Overdose Dose: 5 mg/kg Route: oral Route: single Dose: 5 mg/kg Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS	Other AEs: Heart rate high, Musculoskeletal pain... Other AEs: Heart rate high Musculoskeletal pain (grade 1-2) Headaches Sinus tachycardia Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS
200 mg 3 times / week multiple, oral Recommended Dose: 200 mg, 3 times / week Route: oral Route: multiple Dose: 200 mg, 3 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/26846333/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/26846333/	Sources: https://pubmed.ncbi.nlm.nih.gov/26846333/

AEs

AE	Significance	Dose	Population
Headaches		5 mg/kg single, oral Overdose Dose: 5 mg/kg Route: oral Route: single Dose: 5 mg/kg Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS
Heart rate high		5 mg/kg single, oral Overdose Dose: 5 mg/kg Route: oral Route: single Dose: 5 mg/kg Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS
Sinus tachycardia		5 mg/kg single, oral Overdose Dose: 5 mg/kg Route: oral Route: single Dose: 5 mg/kg Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS
Musculoskeletal pain	grade 1-2	5 mg/kg single, oral Overdose Dose: 5 mg/kg Route: oral Route: single Dose: 5 mg/kg Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.medicines.org.uk/emc/product/12835/smpc#UNDESIRABLE_EFFECTS

PubMed

Title	Date	PubMed
Targeting the hypoxia-sensing pathway in clinical hematology.	2014-02	24371328
First-in-class anemia drug takes aim at Amgen's dominion.	2013-11	24213751

Patents

Sample Use Guides

In Vivo Use Guide

The initial study drug dose is 70 mg three times a week (TIW). The dose is subsequently adjusted to achieve and maintain Hb 11±1 g/dL.

Route of Administration: Oral

In Vitro Use Guide

Roxadustat (5 uM) increases the differentiation of ADMSCs in hypoxic conditions.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 21:36:42 GMT 2025` Edited by `admin` on `Mon Mar 31 21:36:42 GMT 2025`
Record UNII	X3O30D9YMX
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ROXADUSTAT

Official Name

English

roxadustat [INN]

Preferred Name

English

ASP-1517

Code

English

N-[(4-Hydroxy-1-methyl-7-phenoxyisoquinolin-3-yl)carbonyl]glycine

Systematic Name

English

ROXADUSTAT [USAN]

Common Name

English

(((4-HYDROXY-1-METHYL-7-PHENOXYISOQUINOLIN-3-YL)CARBONYL)AMINO)ACETIC ACID

Systematic Name

English

Roxadustat [WHO-DD]

Common Name

English

ROXADUSTAT [JAN]

Common Name

English

FG-4592

Code

English

ASP1517

Code

English

GLYCINE, N-((4-HYDROXY-1-METHYL-7-PHENOXY-3-ISOQUINOLINYL)CARBONYL)-

Systematic Name

English

FG4592

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C471