VABORBACTAM

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C12H16BNO5S
Molecular Weight	297.135
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OB1O[C@H](CC(O)=O)CC[C@@H]1NC(=O)CC2=CC=CS2

InChI

InChIKey=IOOWNWLVCOUUEX-WPRPVWTQSA-N

InChI=1S/C12H16BNO5S/c15-11(7-9-2-1-5-20-9)14-10-4-3-8(6-12(16)17)19-13(10)18/h1-2,5,8,10,18H,3-4,6-7H2,(H,14,15)(H,16,17)/t8-,10-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/28848018 |https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209776lbl.pdf

Vaborbactam (formerly RPX7009) is a new beta-lactamase inhibitor based on a cyclic boronic acid pharmacophore. Vaborbactam is a highly active beta-lactamase inhibitor that restores activity of meropenem and other beta-lactam antibiotics in beta-lactamase-producing bacteria, particularly KPC-producing CRE. Meropenem in combination with vaborbactam (VABOMERE) is indicated for the treatment of patients 18 years and older with complicated urinary tract infections including pyelonephritis caused by designated susceptible bacteria. The vaborbactam component of VABOMERE is a non-suicidal beta-lactamase inhibitor that protects meropenem from degradation by certain serine beta-lactamases such as Klebsiella pneumoniae carbapenemase (KPC). Vaborbactam does not have any antibacterial activity. Vaborbactam does not decrease the activity of meropenem against meropenem-susceptible organisms.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
beta-lactamase activity 2 Target ID: GO:0008800 Sources: https://www.ncbi.nlm.nih.gov/pubmed/28848018	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Urinary tract infections 205 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/209776lbl.pdf	Curative		Approved 8429	VABOMERE Approved Use VABOMERE (meropenem and vaborbactam) is a combination of meropenem, a penem antibacterial, and vaborbactam, a beta-lactamase inhibitor, indicated for the treatment of patients 18 years and older with complicated urinary tract infections (cUTI) including pyelonephritis caused by designated susceptible bacteria. Launch Date 2017
Pneumonia 90 Sources: http://adisinsight.springer.com/drugs/800039513	Curative		Phase III 656	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
33.4 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1500 mg 3 times / day multiple, intravenous dose: 1500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
40.9 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	2000 mg 3 times / day multiple, intravenous dose: 2000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
4.81 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	250 mg 3 times / day multiple, intravenous dose: 250 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.3 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1000 mg 3 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
27.8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1250 mg single, intravenous dose: 1250 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
32.9 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1500 mg single, intravenous dose: 1500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
41.6 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	2000 mg single, intravenous dose: 2000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5.03 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	250 mg single, intravenous dose: 250 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
9.97 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
15.3 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	750 mg single, intravenous dose: 750 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
21.8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
118 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1500 mg 3 times / day multiple, intravenous dose: 1500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
145 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	2000 mg 3 times / day multiple, intravenous dose: 2000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	250 mg 3 times / day multiple, intravenous dose: 250 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
74.6 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1000 mg 3 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
100 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1250 mg single, intravenous dose: 1250 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
114 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1500 mg single, intravenous dose: 1500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
144 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	2000 mg single, intravenous dose: 2000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
16.6 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	250 mg single, intravenous dose: 250 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
35.6 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
51.8 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	750 mg single, intravenous dose: 750 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
79.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
1.65 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1500 mg 3 times / day multiple, intravenous dose: 1500 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.66 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	2000 mg 3 times / day multiple, intravenous dose: 2000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.17 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	250 mg 3 times / day multiple, intravenous dose: 250 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.43 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1000 mg 3 times / day multiple, intravenous dose: 1000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.32 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1250 mg single, intravenous dose: 1250 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.4 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1500 mg single, intravenous dose: 1500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.51 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	2000 mg single, intravenous dose: 2000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.17 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	250 mg single, intravenous dose: 250 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.35 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	500 mg single, intravenous dose: 500 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.24 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	750 mg single, intravenous dose: 750 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1.41 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	1000 mg single, intravenous dose: 1000 mg route of administration: Intravenous experiment type: SINGLE co-administered:	VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
67% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27527080	250 mg single, intravenous dose: 250 mg route of administration: Intravenous experiment type: SINGLE co-administered:		VABORBACTAM plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
2 g 3 times / day multiple, intravenous Recommended Dose: 2 g, 3 times / day Route: intravenous Route: multiple Dose: 2 g, 3 times / day Co-administed with:: Meropenem(2 g; 3 per day for 2 days) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf Page: 2017/209776Orig1s000ClinPharmR.pdf - p.132	healthy, adult n = 26 Health Status: healthy Age Group: adult Population Size: 26 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf Page: 2017/209776Orig1s000ClinPharmR.pdf - p.132	Disc. AE: Chest discomfort... AEs leading to discontinuation/dose reduction: Chest discomfort (3.8%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf Page: 2017/209776Orig1s000ClinPharmR.pdf - p.132
2 g 3 times / day multiple, intravenous Recommended Dose: 2 g, 3 times / day Route: intravenous Route: multiple Dose: 2 g, 3 times / day Co-administed with:: Meropenem(2 g; 3 per day up to 14 days) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192	unhealthy, adult n = 295 Health Status: unhealthy Age Group: adult Sex: M+F Population Size: 295 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192	Disc. AE: Pyrexia, Drug hypersensitivity... AEs leading to discontinuation/dose reduction: Pyrexia (0.3%) Drug hypersensitivity (0.3%) Hypersensitivity (0.3%) Septic shock (0.3%) Infusion related reaction (0.7%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192
2 g 3 times / day multiple, intravenous Highest studied dose\|Recommended Dose: 2 g, 3 times / day Route: intravenous Route: multiple Dose: 2 g, 3 times / day Co-administed with:: Meropenem(2 g; 3 per day for 5 days) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf Page: 209776Orig1s000ClinPharmR.pdf - p.147	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf Page: 209776Orig1s000ClinPharmR.pdf - p.147	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf Page: 209776Orig1s000ClinPharmR.pdf - p.147

AEs

AE	Significance	Dose	Population
Chest discomfort	3.8% Disc. AE	2 g 3 times / day multiple, intravenous Recommended Dose: 2 g, 3 times / day Route: intravenous Route: multiple Dose: 2 g, 3 times / day Co-administed with:: Meropenem(2 g; 3 per day for 2 days) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf Page: 2017/209776Orig1s000ClinPharmR.pdf - p.132	healthy, adult n = 26 Health Status: healthy Age Group: adult Population Size: 26 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf Page: 2017/209776Orig1s000ClinPharmR.pdf - p.132
Drug hypersensitivity	0.3% Disc. AE	2 g 3 times / day multiple, intravenous Recommended Dose: 2 g, 3 times / day Route: intravenous Route: multiple Dose: 2 g, 3 times / day Co-administed with:: Meropenem(2 g; 3 per day up to 14 days) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192	unhealthy, adult n = 295 Health Status: unhealthy Age Group: adult Sex: M+F Population Size: 295 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192
Hypersensitivity	0.3% Disc. AE	2 g 3 times / day multiple, intravenous Recommended Dose: 2 g, 3 times / day Route: intravenous Route: multiple Dose: 2 g, 3 times / day Co-administed with:: Meropenem(2 g; 3 per day up to 14 days) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192	unhealthy, adult n = 295 Health Status: unhealthy Age Group: adult Sex: M+F Population Size: 295 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192
Pyrexia	0.3% Disc. AE	2 g 3 times / day multiple, intravenous Recommended Dose: 2 g, 3 times / day Route: intravenous Route: multiple Dose: 2 g, 3 times / day Co-administed with:: Meropenem(2 g; 3 per day up to 14 days) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192	unhealthy, adult n = 295 Health Status: unhealthy Age Group: adult Sex: M+F Population Size: 295 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192
Septic shock	0.3% Disc. AE	2 g 3 times / day multiple, intravenous Recommended Dose: 2 g, 3 times / day Route: intravenous Route: multiple Dose: 2 g, 3 times / day Co-administed with:: Meropenem(2 g; 3 per day up to 14 days) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192	unhealthy, adult n = 295 Health Status: unhealthy Age Group: adult Sex: M+F Population Size: 295 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192
Infusion related reaction	0.7% Disc. AE	2 g 3 times / day multiple, intravenous Recommended Dose: 2 g, 3 times / day Route: intravenous Route: multiple Dose: 2 g, 3 times / day Co-administed with:: Meropenem(2 g; 3 per day up to 14 days) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192	unhealthy, adult n = 295 Health Status: unhealthy Age Group: adult Sex: M+F Population Size: 295 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000MedR.pdf Page: 209776Orig1s000MedR.pdf - p.192

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inhibitor 1587 inducer 781	inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2B6 810 CYP2C8 911 CYP2C19 1478 P-gp 1461 BCRP 699 OAT1 599 OAT3 642 OCT1 512 OCT2 647 OATP1B1 788 OATP1B3 706 BSEP 402	OAT1 326 OAT3 339 OCT2 355 BCRP 561	CYP1A2 701 CYP2B6 547

Drug as perpetrator

Target	Modality	Activity
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
BSEP 403	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=27 Page: 27.0	no

Drug as victim

Target	Modality	Activity
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=26 Page: 26.0	no
OAT1 326	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=26 Page: 26.0	no
OAT3 339	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=26 Page: 26.0	no
OCT2 355	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000ClinPharmR.pdf#page=26 Page: 26.0	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2017/209776Orig1s000PharmR.pdf#page=31 Page: 31.0

Sourcing

Vendor/Aggregator	ID	URL
AA Blocks	AA01EGKW	https://www.aablocks.com/goods/Goods/detail?id=AA01EGKW
Chem Scene	CS-6445	http://www.chemscene.com/1360457-46-0.html
Chemspace	CSSB00025757703	https://chem-space.com/CSSB00025757703
DC Chemicals	DC10286	http://www.dcchemicals.com//product_show-Vaborbactam.html
Excenen	EX-A2589	https://www.excenen.com/searchresultlist.php?id=1360457-46-0
MedChem Express	HY-19930	https://www.medchemexpress.com/Vaborbactam.html
Smolecule	S546504	http://www.smolecule.com/products/s546504
Synblock Inc	SB17184	http://www.synblock.com/product/1360457-46-0.html
THE BioTek	bt-285457	https://www.thebiotek.com/product/inhibitors/bt-285457
abcr GmbH	AB534390	http://www.abcr.com/shop/en/AB534390
eNovation Chemicals	D572906	http://www.enovationchem.com/productDetails.asp?productID=D572906
eNovation Chemicals	D666960	https://www.enovationchem.com/ProductDetails.asp?ProductID=D666960
iChemical	EBD4042290	http://www.ichemical.com/products/1360457-46-0.html?utm_source=PubChem&utm_medium=website&utm_campaign=product%20catalogs

PubMed

Title	Date	PubMed
Effect of the β-Lactamase Inhibitor Vaborbactam Combined with Meropenem against Serine Carbapenemase-Producing Enterobacteriaceae.	2016 Sep	27381386
Vaborbactam: Spectrum of Beta-Lactamase Inhibition and Impact of Resistance Mechanisms on Activity in Enterobacteriaceae.	2017 Nov	28848018

Patents

Sample Use Guides

In Vivo Use Guide

Administer VABOMERE 4 grams (meropenem 2 grams and vaborbactam 2 grams) every 8 hours by intravenous infusion over 3 hours for up to 14 days, in patients 18 years of age and older with an estimated glomerular filtration rate (eGFR) ≥50 mL/min/1.73m2 Dosage adjustment is recommended in patients with renal impairment who have an eGFR less than 50 mL/min/ 1.73m2

Route of Administration: Intravenous

In Vitro Use Guide

The activity of meropenem combined with the serine β-lactamase inhibitor vaborbactam (formerly RPX7009) was studied against 315 serine carbapenemase-producing Enterobacteriaceae (CPE) isolates by use of checkerboard-designed panels to assess the optimal inhibitor concentration (range tested, 0.5 to 32 μg/ml). Overall, meropenem alone (MIC50 and MIC90, 16 and >64 μg/ml, respectively) inhibited only 2.2% of the isolates at ≤1 μg/ml (the CLSI susceptibility breakpoint) and 7.3% of the isolates at ≤2 μg/ml (the EUCAST breakpoint). Vaborbactam restored meropenem activity for 72.7 to 98.1% of CPE isolates at ≤2 μg/ml, and maximum potentiation was achieved with fixed concentrations of ≥8 μg/ml of the inhibitor (≥96.5% of isolates were inhibited at ≤2 μg/ml of meropenem-vaborbactam). Meropenem-vaborbactam with a fixed concentration of 8 μg/ml of the inhibitor (MIC50, ≤0.06 μg/ml for all organisms) inhibited 93.7% of the CPE isolates displaying elevated meropenem MICs at ≤1 μg/ml. Meropenem-vaborbactam MICs were elevated for isolates producing metallo-β-lactamases (MIC, 16 to >64 μg/ml) or displaying decreased expression of OmpK37 and/or elevated expression of the AcrAB-TolC efflux system (MIC, 16 μg/ml). Vaborbactam showed no antibacterial activity alone (all MICs, >64 μg/ml).

Name

Type

Language

VABORBACTAM

Official Name

English

VABORBACTAM [USAN]

Common Name

English

RPX-7009

Code

English

VABORBACTAM [ORANGE BOOK]

Common Name

English

1,2-OXABORINANE-6-ACETIC ACID, 2-HYDROXY-3-((2-(2-THIENYL)ACETYL)AMINO)-, (3R,6S)-

Systematic Name

English

Vaborbactam [WHO-DD]

Common Name

English

RPX7009

Code

English

CARBAVANCE COMPONENT VABORBACTAM

Brand Name

English

VABORBACTAM COMPONENT OF CARBAVANCE

Brand Name

English

VABOMERE COMPONENT VABORBACTAM

Brand Name

English

vaborbactam [INN]

Common Name

English

VABORBACTAM [MI]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C471