VOXELOTOR

US Previously Marketed

First approved in 2019

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H19N3O3
Molecular Weight	337.3725
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)N1N=CC=C1C2=C(COC3=CC=CC(O)=C3C=O)C=CC=N2

InChI

InChIKey=FWCVZAQENIZVMY-UHFFFAOYSA-N

InChI=1S/C19H19N3O3/c1-13(2)22-16(8-10-21-22)19-14(5-4-9-20-19)12-25-18-7-3-6-17(24)15(18)11-23/h3-11,13,24H,12H2,1-2H3

HIDE SMILES / InChI

Molecular Formula	C19H19N3O3
Molecular Weight	337.3725
Charge	0
Count

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

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27605087 | https://sicklecellanemianews.com/voxelotor-gbt440-for-sickle-cell-anemia/ | https://clinicaltrials.gov/ct2/results?cond=&term=voxelotor&cntry=&state=&city=&dist= | https://www.ncbi.nlm.nih.gov/pubmed/29352729

GBT440 (previously GTx011) is a potent and direct drug for sickle cell treatment. In sickle cell anemia, abnormal hemoglobin molecules are formed, which causes problems for the flow of blood and oxygen through the body. GBT440 can selectively bind to hemoglobin, thereby increasing its affinity for oxygen. By inhibiting hemoglobin polymerization, it also prevents deformation of the red blood cells. GBT440, renamed Voxelotor, is thought to help prevent sickle cells blocking blood vessels, and therefore reduces pain (sickle cell crisis) experienced by patients. GBT440 is well absorbed following intravenous and oral administration, and quickly partitions into the red blood cell with a small part re‐distributed into the plasma. GBT440 was well tolerated in a randomized, placebo‐controlled, double blind, parallel group phase I/II study in healthy volunteers and sickle cell disease patients. Headache is the most reported adverse event related to the use of this drug, and no serious adverse events are known. A phase 3 clinical trial examining the efficacy and safety of the drug (compared to placebo) is planned to be completed in 2019. Voxelotor was also studied as a potential therapy for treatment of low oxygen levels in the blood of idiopathic pulmonary fibrosis patients, but this program was discontinued because of a lack of clinical benefits.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Hemoglobin beta chain 1 Target ID: CHEMBL4331 Sources: https://www.gbt.com/pipeline/sickle-cell-disease/\|https://www.ncbi.nlm.nih.gov/pubmed/29352729\|https://www.ncbi.nlm.nih.gov/pubmed/27378309	Modulator 846

C_max

Value	Dose	Analyte	Population
136 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.21 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
146 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.94 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
225 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.91 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
688 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.4 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
15800 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
166 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10000 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
134 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4950 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
56.6 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
14000 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
215 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
61.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
49.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	1000 mg single, oral dose: 1000 mg route of administration: Oral experiment type: SINGLE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
80.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	300 mg 1 times / day steady-state, oral dose: 300 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
85.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/30743314/	900 mg 1 times / day steady-state, oral dose: 900 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	VOXELOTOR red blood cells	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
1500 mg 1 times / day steady, oral Recommended Dose: 1500 mg, 1 times / day Route: oral Route: steady Dose: 1500 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/213137s000lbl.pdf	unhealthy, 12-59 years Health Status: unhealthy Age Group: 12-59 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/213137s000lbl.pdf	Other AEs: Headache, Diarrhea... Other AEs: Headache (grade 1-2, 26%) Diarrhea (grade 1-2, 19%) Abdominal pain (grade 1-2, 19%) Upper abdominal pain (grade 1-2, 19%) Nausea (grade 1-2, 16%) Fatigue (grade 1-2, 14%) Rash (grade 1-2, 13%) Urticaria (grade 1-2, 14%) Generalized rash (grade 1-2, 10%) Maculo-papular rash (grade 1-2, 14%) Pruritic rash (grade 1-2, 14%) Papular rash (grade 1-2, 14%) Erythematous rash (grade 1-2, 14%) Vesicular rash (grade 1-2, 14%) Pyrexia (grade 1-2, 12%) Diarrhea (grade 3, 1 patient) Nausea (grade 3, 1 patient) Rash (grade 3, 1 patient) Generalized rash (grade 3, 3 patients) Headache (serious, 1 patient) Hypersensitivity (serious, 1 patient) Pulmonary embolism (serious, 1 patient) Headache (>1 patient) Diarrhea (>1 patient) Rash (>1 patient) Vomiting (2.3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/213137s000lbl.pdf
1500 mg 1 times / day steady, oral Recommended Dose: 1500 mg, 1 times / day Route: oral Route: steady Dose: 1500 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf	unhealthy, 12-59 years Health Status: unhealthy Age Group: 12-59 years Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf	Disc. AE: Sickle cell anemia with crisis, Nausea... Other AEs: Sickle cell anemia with crisis, Abdominal pain... AEs leading to discontinuation/dose reduction: Sickle cell anemia with crisis (2.3%) Nausea (1.1%) Chest pain (1.1%) Angina pectoris (1.1%) Paresthesia (1.1%) Pneumonia (1.1%) Pulmonary embolism (1.1%) Pulmonary sepsis (1.1%) Abdominal pain (1.1%) Other AEs: Sickle cell anemia with crisis (19.3%) Abdominal pain (1 patient) Acute chest syndrome (5.7%) Diarrhea (3.4%) Rash (2.3%) Sickle cell anemia with crisis (2.3%) Generalized rash (2.3%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf
2800 mg single, oral Highest studied dose Dose: 2800 mg Route: oral Route: single Dose: 2800 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf	healthy Health Status: healthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf
1000 mg steady, oral Recommended Dose: 1000 mg Route: oral Route: steady Dose: 1000 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252	inhibitor 2438 inducer 440 substrate 1193	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2C19 2057 CYP2C8 1057 BCRP 910 P-gp 1741 OATP1B1 1079 OATP1B3 961 OCT2 779 OAT1 725 OAT3 747 MATE1 415 MATE2 267 BSEP 550	OATP1A2 67 OATP1B1 503 OATP1B3 435 BSEP 63 OAT1 395 OAT3 391 OCT2 434 MATE1 182 MATE2 98 CYP2C19 1119 CYP2B6 776	CYP1A2 832 CYP2C19 329 CYP3A4/5 133 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	likely
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211	no [Ki 0.8 uM]	no (co-administration study) Comment: administered with rosiglitazone, no effect on rosiglitazone was observed Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211	no [Ki 11.1 uM]	no (co-administration study) Comment: administered with omeprazole, no effect on omeprazole was observed Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211	no [Ki 35 uM]	no (co-administration study) Comment: administered with caffeine, no effect on caffeine exposure was observed Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211	no [Ki 9.5 uM]	no (co-administration study) Comment: administered with warfarin, no effect on warfarin exposure was observed Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211	no [Ki 96.1 uM]	no (co-administration study) Comment: administered with metoprolol, no effect on metoprolol was observed Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95;211
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
CYP3A4/5 357	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
MATE2 267	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no	no (co-administration study) Comment: administered with caffeine, no effect on caffeine exposure was observed; did not cause concentration-dependent increases in mRNA levels Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no	no (co-administration study) Comment: administered with omeprazole, no effect on omeprazole was observed Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no	no (co-administration study) Comment: administered with warfarin, no effect on warfarin exposure was observed Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	weak	no (co-administration study) Comment: AUC and Cmax of digoxin (a P-gp substrate) increased by only 12% and 17%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=106 Page: 106.0	yes	yes (co-administration study) Comment: midazolam exposure increased by 63% and the metabolite hydroxymidazolam increased by 75% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=106 Page: 106.0

Drug as victim

Target	Modality	Activity
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=105 Page: 105.0	major
CYP2B6 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=105 Page: 105.0	minor
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=105 Page: 105.0	minor
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=105 Page: 105.0	minor
BSEP 63	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
MATE1 182	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
MATE2 98	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OATP1A2 67	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=95 Page: 95.0	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2019/213137Orig1s000Multidiscipline.pdf#page=57 Page: 57.0

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY447663	https://www.001chemical.com/chem/1446321-46-5
AA Blocks	AA00ABL8	https://www.aablocks.com/goods/Goods/detail?id=AA00ABL8
Aaron Chemicals	AR00ACD0	http://www.aaronchem.com/1446321-46-5
AbMole Bioscience	M9778	http://www.abmole.com/products/voxelotor.html
Angel Pharmatech	AG303307	http://www.angelpharmatech.com/1446321-46-5.html
Ark Pharm	AK547400	http://www.arkpharminc.com/products/1446321-46-5.html
Ark Pharma Scientific Limited	H-022273	http://www.arkpharmtech.com/product/27327.html
BioChemPartner	BCP20182	http://www.biochempartner.com/1446321-46-5-BCP20182
BOC Sciences	1446321-46-5	https://www.bocsci.com/gbt-440-cas-1446321-46-5-item-474581.html
Chem Scene	CS-5317	http://www.chemscene.com/1446321-46-5.html
Chemspace	CSSB00025757729	https://chem-space.com/CSSB00025757729
DC Chemicals	DC10474	http://www.dcchemicals.com/product_show-GBT440.html
Debye Scientific	DA-44587	http://www.debyesci.com/cas_1446321-46-5.html
eNovation Chemicals	D677141	https://www.enovationchem.com/ProductDetails.asp?ProductID=D677141
eNovation Chemicals	D762780	https://www.enovationchem.com/ProductDetails.asp?ProductID=D762780
eNovation Chemicals	Y0998128	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y0998128
eNovation Chemicals	Y1012667	https://www.enovationchem.com/ProductDetails.asp?ProductID=Y1012667
Excenen	EX-A2980	https://www.excenen.com/searchresultlist.php?id=1446321-46-5
Finetech	FT-0702904	http://www.finetechnology-ind.com/prod/detail/pub/1446321-46-5.html
Lab Network	LN01343613	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01343613
MedChem Express	HY-18681	https://www.medchemexpress.com/GBT-440.html
Molcore	MC447663	https://www.molcore.com/product/1446321-46-5
Smolecule	S546872	http://www.smolecule.com/products/s546872
Synblock Inc	SB19656	http://www.synblock.com/product/1446321-46-5.html
THE BioTek	bt-286495	https://www.thebiotek.com/product/inhibitors/bt-286495

Substance Class	Chemical Created by `admin` on `Mon Mar 31 22:55:25 GMT 2025` Edited by `admin` on `Mon Mar 31 22:55:25 GMT 2025`
Record UNII	3ZO554A4Q8
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

VOXELOTOR

Official Name

English

voxelotor [INN]

Preferred Name

English

VOXELOTOR [MI]

Common Name

English

VOXELOTOR [ORANGE BOOK]

Common Name

English

VOXELOTOR [USAN]

Common Name

English

OXBRYTA

Brand Name

English

BENZALDEHYDE, 2-HYDROXY-6-((2-(1-(1-METHYLETHYL)-1H-PYRAZOL-5-YL)-3-PYRIDINYL)METHOXY)-

Systematic Name

English

GTX-011

Code

English

2-HYDROXY-6-((2-(1-ISOPROPYL-1H-PYRAZOL-5-YL)PYRIDIN-3-YL)METHOXY) BENZALDEHYDE

Systematic Name

English

GBT440

Code

English

Voxelotor [WHO-DD]

Common Name

English

GBT-440

Code

English

Classification Tree Code System Code

NCI_THESAURUS

C78275