IBREXAFUNGERP PHOSPHATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C44H67N5O4.H3O4P
Molecular Weight	828.0291
Optical Activity	UNSPECIFIED
Defined Stereocenters	12 / 12
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

OP(O)(O)=O.CC(C)[C@@H](C)[C@@]1(C)CC[C@]2(C)[C@H]3CC[C@H]4[C@]5(C)COC[C@@]4(C[C@H]([C@@H]5OC[C@](C)(N)C(C)(C)C)N6N=CN=C6C7=CC=NC=C7)C3=CC[C@@]2(C)[C@@H]1C(O)=O

InChI

InChIKey=OAKUEXTYOMFKTF-FQGZCCSZSA-N

InChI=1S/C44H67N5O4.H3O4P/c1-27(2)28(3)39(7)18-19-41(9)30-12-13-33-40(8)23-52-25-44(33,31(30)14-17-42(41,10)34(39)37(50)51)22-32(35(40)53-24-43(11,45)38(4,5)6)49-36(47-26-48-49)29-15-20-46-21-16-29;1-5(2,3)4/h14-16,20-21,26-28,30,32-35H,12-13,17-19,22-25,45H2,1-11H3,(H,50,51);(H3,1,2,3,4)/t28-,30+,32-,33+,34-,35+,39-,40-,41-,42+,43+,44+;/m1./s1

HIDE SMILES / InChI

Molecular Formula	H3O4P
Molecular Weight	97.9952
Charge	0
Count

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

Molecular Formula	C44H67N5O4
Molecular Weight	730.0339
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	12 / 12
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25896696 | https://www.ncbi.nlm.nih.gov/pubmed/25512406 | https://www.ncbi.nlm.nih.gov/pubmed/24323472 | https://www.ncbi.nlm.nih.gov/pubmed/23190764https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214900s001lbl.pdf

Ibrexafungerp (BREXAFEMME®) is an orally active triterpenoid antifungal drug being developed by SCYNEXIS, Inc. for the treatment of fungal infections. The inhibition of β-1,3-D glucan synthetase by ibrexafungerp compromises the integrity of fungal cell walls. Ibrexafungerp has been recently approved for the treatment of vulvovaginal candidiasis (VVC), and it is the first novel antifungal drug class to be approved in more than 20 years. Food and Drug Administration's decision was based on positive results from two pivotal phase III studies in which oral ibrexafungerp proved both safe and effective in patients with vulvovaginal candidiasis. Development for the treatment of recurrent VVC and invasive fungal infections is ongoing.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
1,3-beta-glucan synthase 10 Target ID: CHEMBL2364673 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214900s001lbl.pdf\|https://pubmed.ncbi.nlm.nih.gov/32854252\|https://pubmed.ncbi.nlm.nih.gov/33668824	Inhibitor 8504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Vulvovaginal candidiasis 13 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214900s001lbl.pdf	Curative		Approved 8583	BREXAFEMME Approved Use Indicated for the treatment of adult and post-menarchal pediatric females with vulvovaginal candidiasis Launch Date 2021

C_max

Value	Dose	Analyte	Population
420.6 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=84	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
318 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=84	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
36.13 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=87 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=200	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6.13 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.75 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
30.87 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
60.24 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
71.93 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
167.86 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
349.15 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
875.86 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
895.6 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2085.4 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	1600 mg single, oral dose: 1600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
308.6 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
553.7 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
705.9 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1272 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1024 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1609 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1112 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
2634 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
724.1 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=182	750 mg 2 times / day multiple, oral dose: 750 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1497 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=182	750 mg 1 times / day multiple, oral dose: 750 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1542 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=183	600 mg 3 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
1196 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=183	500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
959 nM OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=183	500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
11052 nM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=84	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
7997 nM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=84	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
795.1 nM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=87 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=200	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.15 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.26 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.62 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.33 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.7 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
3.27 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.27 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
17.97 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
20.07 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
51.6 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	1600 mg single, oral dose: 1600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.82 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
9.01 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
9.38 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
21.11 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
12.53 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
26.38 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
13.75 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
45.85 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
6283 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=182	750 mg 2 times / day multiple, oral dose: 750 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
15630 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=182	750 mg 1 times / day multiple, oral dose: 750 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
20.75 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=183	600 mg 3 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
20.95 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=183	500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
16.11 μM × h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=183	500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
20 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=80	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
20.3 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=87 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=200	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
21 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
16.4 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
17.8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
21.1 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
19.9 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	80 mg single, oral dose: 80 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
19.7 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
20.5 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	300 mg single, oral dose: 300 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
18.7 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
19.3 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	800 mg single, oral dose: 800 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
20.9 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=179	1600 mg single, oral dose: 1600 mg route of administration: Oral experiment type: SINGLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
13.3 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
24.7 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	300 mg 1 times / day multiple, oral dose: 300 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
14.6 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
28.9 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	600 mg 1 times / day multiple, oral dose: 600 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
11.3 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
32.3 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
14.3 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day multiple, oral dose: 800 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
22.6 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=180	800 mg 1 times / day steady-state, oral dose: 800 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
41.071 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=182	750 mg 1 times / day multiple, oral dose: 750 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
19.3 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=183	500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
25.6 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=183	500 mg 1 times / day multiple, oral dose: 500 mg route of administration: Oral experiment type: MULTIPLE co-administered:	IBREXAFUNGERP plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.187% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=186			IBREXAFUNGERP plasma	Homo sapiens population: age: UNKNOWN sex: UNKNOWN food status:

Doses

Dose	Population	Adverse events
1600 mg single, oral MTD Dose: 1600 mg Route: oral Route: single Dose: 1600 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf	Disc. AE: Abdominal pain... AEs leading to discontinuation/dose reduction: Abdominal pain (serious, 1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf
750 mg single, oral Studied dose Dose: 750 mg Route: oral Route: single Dose: 750 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf	Disc. AE: Gastrointestinal events, Dizziness... AEs leading to discontinuation/dose reduction: Gastrointestinal events (2 patients) Dizziness (1 patient) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf

AEs

AE	Significance	Dose	Population
Abdominal pain	serious, 1 patient Disc. AE	1600 mg single, oral MTD Dose: 1600 mg Route: oral Route: single Dose: 1600 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf
Dizziness	1 patient Disc. AE	750 mg single, oral Studied dose Dose: 750 mg Route: oral Route: single Dose: 750 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf
Gastrointestinal events	2 patients Disc. AE	750 mg single, oral Studied dose Dose: 750 mg Route: oral Route: single Dose: 750 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 1087 substrate 1946 inhibitor 2252	inhibitor 2438 substrate 1193	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 620 OAT3 747 CYP1A2 2153 CYP2B6 926 BSEP 550 CYP2C19 2057 BCRP 910 OCT2 779 UGT1A1 246 UGT1A3 89 UGT2B15 84 CYP2C8 1057 UGT2B7 197 UGT1A9 148 UGT1A6 136 UGT1A4 98 OAT1 725 MATE2-K 77 MRP2 499 OATP1B3 961 OATP1B1 1079 P-gp 1741 MATE1 415	CYP3A5 446 P-gp 2052 CYP2C8 810 OAT3 391 MRP2 252 BCRP 697 OATP1B1 503 UGT1A3 470 UGT1A1 479 UGT1A4 399 UGT1A6 343 UGT1A8 323 UGT1A9 423 UGT1A10 331 UGT2B7 456 UGT2B17 237 OCT2 434 OATP1B3 435 OAT1 395 MATE1 182 MATE2-K 33	CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=44 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=89 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=192 Page: 44 \| 50 \| 83 \| 89 \| 192 \| 204	moderate [IC50 7.2 uM]	yes (co-administration study) Comment: Increased tacrolimus AUCinf by 1.4-fold but no effect on Cmax Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=44 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=89 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=192 Page: 44 \| 50 \| 83 \| 89 \| 192 \| 204
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=192 Page: 50 \| 192	no [IC50 26 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=192 Page: 50 \| 192	no [IC50 41 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=192 Page: 50 \| 192	no [IC50 60 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=192 Page: 50 \|192	no [IC50 >100 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=192 Page: 50 \| 192	no [IC50 >100 uM]
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 198	no [IC50 >30 uM]
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 198	no [IC50 >30 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 198	no [IC50 >30 uM]
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 198	no [IC50 >30 uM]
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 198	no [IC50 >30 uM]
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=44 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=194 Page: 44 \| 50 \| 194	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=195 Page: 195.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=44 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=196 Page: 44 \| 50 \| 196	no
UGT1A9 155	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=197 Page: 197.0	no
UGT1A6 171	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=197 Page: 197.0	weak [IC50 >100 uM]
UGT2B7 210	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=197 Page: 197.0	weak [IC50 >100 uM]
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=89 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 89 \| 198 \| 207	yes [IC50 0.335 uM]	yes (co-administration study) Comment: Increased pravastatin AUC24 and Cmax by 2.8-fold and 3.5-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=89 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 89 \| 198 \| 207
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=44 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=192 Page: 44 \| 50 \| 83 \| 192 \| 205	yes [IC50 1.5 uM]	no (co-administration study) Comment: No change in AUCinf or Cmax of rosiglitazone Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=44 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=50 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=192 Page: 44 \| 50 \| 83 \| 192 \| 205
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=89 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 89 \| 198 \| 206	yes [IC50 1.64 uM]	yes (co-administration study) Comment: Increased dabigatran AUC48 and Cmax by 1.4-fold and 1.25-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=89 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 89 \| 198 \| 206
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 198	yes [IC50 11.5 uM]
UGT1A3 99	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=197 Page: 197.0	yes [IC50 19.5 uM]
UGT2B15 84	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=197 Page: 197.0	yes [IC50 2.19 uM]
MRP2 625	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 198	yes [IC50 20.9 uM]
UGT1A1 303	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=197 Page: 197.0	yes [IC50 26.2 uM]
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 198	yes [IC50 3.91 uM]
UGT1A4 100	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=197 Page: 197.0	yes [IC50 9.84 uM]
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=199 Page: 199.0	yes
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=199 Page: 199.0	yes

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP3A5 446	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=80 Page: 80.0	minor
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 198.0	no
MATE1 182	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 198.0	no
MATE2-K 33	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 198.0	no
MRP2 252	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 198.0	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 198.0	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 198.0	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 198.0	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 198.0	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 198.0	no
UGT1A1 479	substrate 4014 Sources: \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	no
UGT1A10 331	substrate 4014 Sources: \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	no
UGT1A4 399	substrate 4014 Sources: \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	no
UGT1A6 343	substrate 4014 Sources: \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	no
UGT1A8 323	substrate 4014 Sources: \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	no
UGT1A9 423	substrate 4014 Sources: \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	no
UGT2B17 237	substrate 4014 Sources: \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	no
UGT2B7 456	substrate 4014 Sources: \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	no
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	weak
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=49 Page: 49.0	weak
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=83 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=198 Page: 83 \| 198	yes
UGT1A3 470	substrate 4014 Sources: \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=190 Page: 190.0	yes
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=22 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=49 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=81 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=86 Page: 22 \| 49 \| 81 \| 86 \| 201	yes	yes (co-administration study) Comment: Ketoconazole increased AUC and Cmax by 5.8-fold and 2.5-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=22 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=49 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=81 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=86 Page: 22 \| 49 \| 81 \| 86 \| 201

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2021/214900Orig1s000MultidisciplineR.pdf#page=45 Page: 45.0

PubMed

Title	Date	PubMed
Ibrexafungerp: A new triterpenoid antifungal.	2022-12-05	36083109
Pharmacokinetics and Pharmacodynamics of Ibrexafungerp.	2022-03	34961907
The Antifungal Pipeline: Fosmanogepix, Ibrexafungerp, Olorofim, Opelconazole, and Rezafungin.	2021-10	34626339
Ibrexafungerp: First Approval.	2021-08	34313977
Antifungal activities of SCY-078 (MK-3118) and standard antifungal agents against clinical non-Aspergillus mold isolates.	2015-07	25896696

Patents

Sample Use Guides

In Vivo Use Guide

The recommended dosage of BREXAFEMME in adult and post-menarchal pediatric females is 300 mg (two tablets of 150 mg) twice a day for one day, for a total treatment dosage of 600 mg.

Route of Administration: Oral

In Vitro Use Guide

Ibrexafungerp showed antifungal in vitro activity against the studied isolates. Wild-type upper limits for ibrexafungerp were >0.25 mg/L against C. albicans, >1 mg/L against C. parapsilosis, C. glabrata, and C. tropicalis, and >2 mg/L against C. krusei.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 21:49:34 GMT 2025` Edited by `admin` on `Mon Mar 31 21:49:34 GMT 2025`
Record UNII	76HJ8T68WO
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

MK-3118 PHOSPHATE

Preferred Name

English

IBREXAFUNGERP PHOSPHATE

Common Name

English

SCY-078 PHOSPHATE

Code

English

Code System Code Type Description

CAS

1965291-14-8

Created by admin on Mon Mar 31 21:49:34 GMT 2025 , Edited by admin on Mon Mar 31 21:49:34 GMT 2025

PRIMARY

PUBCHEM

171360806

Created by admin on Mon Mar 31 21:49:34 GMT 2025 , Edited by admin on Mon Mar 31 21:49:34 GMT 2025

PRIMARY

FDA UNII

76HJ8T68WO

Created by admin on Mon Mar 31 21:49:34 GMT 2025 , Edited by admin on Mon Mar 31 21:49:34 GMT 2025

PRIMARY

Related Record Type Details


					A92JFM5XNU

IBREXAFUNGERP

PARENT -> SALT/SOLVATE

Related Record Type Details


					A92JFM5XNU

IBREXAFUNGERP

ACTIVE MOIETY

Details

SMILES

InChI

DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/25896696 | https://www.ncbi.nlm.nih.gov/pubmed/25512406 | https://www.ncbi.nlm.nih.gov/pubmed/24323472 | https://www.ncbi.nlm.nih.gov/pubmed/23190764https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214900s001lbl.pdf

CNS Activity

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

PubMed

Patents

Sample Use Guides

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25896696 | https://www.ncbi.nlm.nih.gov/pubmed/25512406 | https://www.ncbi.nlm.nih.gov/pubmed/24323472 | https://www.ncbi.nlm.nih.gov/pubmed/23190764https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214900s001lbl.pdf

C_max

T_1/2

F_unbound

Drug as perpetrator