Vibegron

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C26H28N4O3
Molecular Weight	444.5255
Optical Activity	UNSPECIFIED
Defined Stereocenters	4 / 4
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O[C@@H]([C@H]1CC[C@@H](CC2=CC=C(NC(=O)[C@@H]3CCC4=NC=CC(=O)N34)C=C2)N1)C5=CC=CC=C5

InChI

InChIKey=DJXRIQMCROIRCZ-XOEOCAAJSA-N

InChI=1S/C26H28N4O3/c31-24-14-15-27-23-13-12-22(30(23)24)26(33)29-19-8-6-17(7-9-19)16-20-10-11-21(28-20)25(32)18-4-2-1-3-5-18/h1-9,14-15,20-22,25,28,32H,10-13,16H2,(H,29,33)/t20-,21+,22-,25+/m0/s1

HIDE SMILES / InChI

Molecular Formula	C26H28N4O3
Molecular Weight	444.5255
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	4 / 4
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213006s000lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/30411311 | https://www.kyorin-gr.co.jp/en/news/docs/57a20666168a4c90f3519957b2d2f928028651b5.pdf | https://www.ncbi.nlm.nih.gov/pubmed/27965369

Vibegron is a selective beta 3 adrenergic receptor (β3AR) agonist that is being developed in Japan jointly by Kyorin Pharmaceutical Co., Ltd and Kissei Pharmaceutical Co., Ltd and in other regions worldwide (except in several other Asian countries) by Urovant Sciences for the treatment of overactive bladder (OAB). Vibegron potently activates human b3AR and increases cAMP levels, with an EC50 of 1.1 nM. Based on results from Japanese phase III trials, vibegron received approval in Japan in September 2018 for this indication. Vibegron, an active ingredient of Beova® Tablets, is a novel once-daily oral treatment for overactive bladder (OAB), acts selectively on the bladder's β3-adrenergic receptor, relaxes the bladder and enhances the urine collection, and consequently improves the symptoms of urgency, urinary frequency and urge urinary incontinence associated with OAB. On December 23, 2020 the FDA approved vibegron (Gemtesa) for the treatment of adult patients with overactive bladder (OAB) with symptoms of urge urinary incontinence (UUI), urgency, and urinary frequency.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Beta-3 adrenergic receptor 54 Target ID: CHEMBL246 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213006s000lbl.pdf \|https://pubmed.ncbi.nlm.nih.gov/26709102	Agonist 2752		1.1 nM [EC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Overactive bladder 39 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213006s000lbl.pdf	Primary		Approved 8583	Gemtesa Approved Use GEMTESA is indicated for the treatment of overactive bladder (OAB) with symptoms of urge urinary incontinence, urgency, and urinary frequency in adults Launch Date 2020

C_max

Value	Dose	Analyte	Population
177 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=33	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.14 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
0.79 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
4.76 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.25 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
31.7 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
50.2 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
142 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
195 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
274 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
618 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
645 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1330 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
106 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=36	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
96.4 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=36	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
15.6 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
41.6 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
169 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
224 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
305 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
276 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
216 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
313 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
733 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1400 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
168 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=42	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
125 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=42	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
342.83 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
404.5 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
473.01 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
240.8 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
23.65 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
63.96 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
81.11 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
114.4 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

AUC

Value	Dose	Analyte	Population
3.51 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=33	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
14.3 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
71.6 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
119 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
542 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
948 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1890 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2280 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3620 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
7380 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9160 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
15500 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.35 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=36	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1.77 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=36	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
164 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
507 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1280 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2230 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2410 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2370 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2560 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3200 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6980 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
10400 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1820 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=42	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
1440 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=42	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
6337.17 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7137.53 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
5156.07 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
3466.04 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
721.9 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
1146 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
1370 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
1524 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

T_1/2

Value	Dose	Analyte	Population
133 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=33	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
45.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
64.1 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
50.4 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
95.1 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
73.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
68.4 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
75.8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	200 mg single, oral dose: 200 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
63.8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
60.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	450 mg single, oral dose: 450 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
60.7 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=35	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
94.9 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	25 mg 1 times / day multiple, oral dose: 25 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
78 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
80.8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
89.4 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
80 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
78.6 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
80.4 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	150 mg 1 times / day multiple, oral dose: 150 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
65.1 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	200 mg 1 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
58.8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
59.4 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=40	400 mg 1 times / day multiple, oral dose: 400 mg route of administration: Oral experiment type: MULTIPLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
94.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=42	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
92.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=42	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
130.6 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
108.2 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
96.2 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
98.8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=45	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
79.42 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
87.2 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
87.86 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
82.35 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=50	75 mg single, oral dose: 75 mg route of administration: Oral experiment type: SINGLE co-administered:	VIBEGRON plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
50% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=5 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10			VIBEGRON plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
600 mg single, oral Highest studied dose Dose: 600 mg Route: oral Route: single Dose: 600 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf	healthy Health Status: healthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf	Other AEs: No toxicities were reported... Other AEs: No toxicities were reported Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf
75 mg 1 times / day steady-state, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: steady-state Dose: 75 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf	Other AEs: No toxicities were reported... Other AEs: No toxicities were reported Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf

AEs

AE	Significance	Dose	Population
No toxicities were reported		600 mg single, oral Highest studied dose Dose: 600 mg Route: oral Route: single Dose: 600 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf	healthy Health Status: healthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf
No toxicities were reported		75 mg 1 times / day steady-state, oral Recommended Dose: 75 mg, 1 times / day Route: oral Route: steady-state Dose: 75 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf	unhealthy Health Status: unhealthy Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf

Overview

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

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP3A5 136 BCRP 910 MATE1 415 OCT1 620 OAT1 725 OCT2 779 OAT3 747 MATE2-K 77 CYP1A2 2153 CYP2B6 926 CYP2C8 1057 P-gp 1741 CYP2C19 2057 OATP1B1 1079 OATP1B3 961	MATE2-K 33 OATP1B1 503 OCT1 393 OCT2 434 OATP1B3 435 BCRP 697 MATE1 182 CYP3A5 446 P-gp 2052	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP3A5 201	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 Page: 11.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=66 Page: 11 \| 66	no	no (co-administration study) Comment: Increased Telterodine AUC24 and Cmax by 8%, 12% (100mg Vibegron QD) or 23%, 37% (150mg Vibegron QD) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=11 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=66 Page: 11 \| 66

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A5 446	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=16 Page: 16.0	minor
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=10 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=16 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=54 Page: 5 \| 10 \| 16 \| 17 \| 54	minor	likely (co-administration study) Comment: Diltiazem or ketoconazole increased Cmax and AUC by 1.68-fold and 1.63-fold or by 1.68-fold and 1.63-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=10 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=16 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=54 Page: 5 \| 10 \| 16 \| 17 \| 54
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
MATE1 182	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
MATE2-K 33	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT1 393	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10 Page: 10.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=6 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=16 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=60 Page: 6 \| 10 \| 16 \| 17 \| 60	yes	yes (co-administration study) Comment: Increased Digoxin Cmax and AUC by 21% and 11%, Diltiazem or ketoconazole increased exposures by >=2-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=6 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=10 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=16 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000ClinPharmR.pdf#page=60 Page: 6 \| 10 \| 16 \| 17 \| 60

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2020/213006Orig1s000PharmR.pdf#page=33 Page: 33 \| 138

PubMed

Title	Date	PubMed
Vibegron: First Global Approval.	2018-11	30411311
Pharmacological Characterization of a Novel Beta 3 Adrenergic Agonist, Vibegron: Evaluation of Antimuscarinic Receptor Selectivity for Combination Therapy for Overactive Bladder.	2017-02	27965369
Discovery of Vibegron: A Potent and Selective β3 Adrenergic Receptor Agonist for the Treatment of Overactive Bladder.	2016-01-28	26709102

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dose is one 75 mg tablet once daily.

Route of Administration: Oral

In Vitro Use Guide

Vibegron potently activates human b3AR and increases cAMP levels, with an EC50 of 1.1 nM and 87% activation relative to isoproterenol. Vibegron is also highly selective over b1AR and b2AR versus b3AR across multiple species, demonstrating >9000-fold selectivity for activation of b3AR over b1AR or b2AR in cell based in vitro functional assays. A small serum shift was observed in the presence of 40% human serum (EC501.7 nM).

Substance Class	Chemical Created by `admin` on `Mon Mar 31 21:34:13 GMT 2025` Edited by `admin` on `Mon Mar 31 21:34:13 GMT 2025`
Record UNII	M5TSE03W5U
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

Vibegron [INN]

Preferred Name

English

Vibegron

Official Name

English

Gemtesa

Brand Name

English

(6S)-N-[4-({(2S,5R)-5-[(R)-Hydroxyphenylmethyl]pyrrolidin-2-yl}methyl)phenyl]-4-oxo-4,6,7,8-tetrahydropyrrolo[1,2-a]pyrimidine-6-carboxamide

Systematic Name

English

Vibegron [WHO-DD]

Common Name

English

Pyrrolo[1,2-a]pyrimidine-6-carboxamide, 4,6,7,8-tetrahydro-N-[4-[[(2S,5R)-5-[(R)-hydroxyphenylmethyl]-2-pyrrolidinyl]methyl]phenyl]-4-oxo-, (6S)-

Systematic Name

English

Vibegron [USAN]

Common Name

English

KRP-114V

Code

English

(6S)-N-(4-(((2S,5R)-5-((R)-hydroxy(phenyl)methyl)pyrrolidin-2-yl(methyl)phenyl)-4-oxo-4,6,7,8-tetrahydropyrrolo(1,2-a)pyrimidine-

Systematic Name

English

(6S)-4,6,7,8-Tetrahydro-N-[4-[[(2S,5R)-5-[(R)-hydroxyphenylmethyl]-2-pyrrolidinyl]methyl]phenyl]-4-oxopyrrolo[1,2-a]pyrimidine-6-carboxamide

Systematic Name

English

Vibegron [JAN]

Common Name

English

Vibegron [ORANGE BOOK]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C48149