MAVACAMTEN

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C15H19N3O2
Molecular Weight	273.3303
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)N1C(=O)NC(N[C@@H](C)C2=CC=CC=C2)=CC1=O

InChI

InChIKey=RLCLASQCAPXVLM-NSHDSACASA-N

InChI=1S/C15H19N3O2/c1-10(2)18-14(19)9-13(17-15(18)20)16-11(3)12-7-5-4-6-8-12/h4-11,16H,1-3H3,(H,17,20)/t11-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214998s000lbl.pdf

Mavacamten (Camzyos™; MYK-461) is an oral small-molecule cardiac myosin inhibitor developed by MyoKardia, Inc., a wholly owned subsidiary of Bristol Myers Squibb, for the treatment of hypertrophic cardiomyopathy (HCM) and diseases of diastolic dysfunction. Mavacamten is an allosteric and reversible inhibitor selective for cardiac myosin. Mavacamten modulates the number of myosin heads that can enter “on actin” (power-generating) states, thus reducing the probability of force-producing (systolic) and residual (diastolic) cross-bridge formation. Excess myosin actin cross-bridge formation and dysregulation of the super-relaxed state are mechanistic hallmarks of HCM. Mavacamten shifts the overall myosin population towards an energy-sparing, recruitable, super-relaxed state. In HCM patients, myosin inhibition with mavacamten reduces dynamic LVOT obstruction and improves cardiac filling pressures. In April 2022, mavacamten was approved for use in the USA in the treatment of adults with symptomatic New York Heart Association (NYHA) class II-III obstructive HCM to improve functional capacity and symptoms.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Cardiac myosin ATPase 1 Target ID: Cardiac myosin ATPase Sources: https://www.ncbi.nlm.nih.gov/pubmed/26912705	Inhibitor 8504		0.3 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Symptomatic New York Heart Association class II-III obstructive hypertrophic cardiomyopathy 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/214998s000lbl.pdf	Primary		Approved 8583	Camzyos Approved Use Indicated for the treatment of adults with symptomatic New York Heart Association (NYHA) class II-III obstructive hypertrophic cardiomyopathy to improve functional capacity and symptoms. Launch Date 2022

C_max

Value	Dose	Analyte	Population
509 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=40	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
397 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=40	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
596 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=41	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
534 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=41	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
468 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=41	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
426 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=41	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
153 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
341.1 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
333 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
490 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
391 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg 1 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
596 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg 1 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
141 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
289 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
504 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
516 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
333.2 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
489.9 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
20.9 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
62 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
101 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
204 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
492 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	24 mg single, oral dose: 24 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
894 ng/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	48 mg single, oral dose: 48 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
43520 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=40	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
14130 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=40	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
71000 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=41	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
18200 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=41	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
32800 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=41	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: FASTED
19700 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=41	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
9395 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: HIGH-FAT
10690 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FASTED
12530 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
42800 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
2768 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg 1 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
8313 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg 1 times / day multiple, oral dose: 15 mg route of administration: Oral experiment type: MULTIPLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
6277 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
15410 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
17370 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
19280 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
12530 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
42800 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
296 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	1 mg single, oral dose: 1 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1368 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	2 mg single, oral dose: 2 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3245 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	6 mg single, oral dose: 6 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
5333 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	12 mg single, oral dose: 12 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
14555 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	24 mg single, oral dose: 24 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
32990 ng × h/mL OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=82	48 mg single, oral dose: 48 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
193 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
553 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
216 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
216 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
141 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
144 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
192.7 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
552.8 h OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=81	15 mg single, oral dose: 15 mg route of administration: Oral experiment type: SINGLE co-administered:	MAVACAMTEN plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
6.9% OTHER GOV'T https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000PharmR.pdf#page=99			MAVACAMTEN plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
20 mg 1 times / day multiple, oral Highest studied dose Dose: 20 mg, 1 times / day Route: oral Route: multiple Dose: 20 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf
5 mg 1 times / day multiple, oral Studied dose Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf	Disc. AE: Atrial fibrillation, Adverse event... AEs leading to discontinuation/dose reduction: Atrial fibrillation (0.8%) Adverse event (2.4%) Syncope (0.8%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf

AEs

AE	Significance	Dose	Population
Atrial fibrillation	0.8% Disc. AE	5 mg 1 times / day multiple, oral Studied dose Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf
Syncope	0.8% Disc. AE	5 mg 1 times / day multiple, oral Studied dose Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf
Adverse event	2.4% Disc. AE	5 mg 1 times / day multiple, oral Studied dose Dose: 5 mg, 1 times / day Route: oral Route: multiple Dose: 5 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000Med_StatR.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inducer 1087 inhibitor 2252	substrate 1193 inducer 440 inhibitor 2438	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
OCT1 620 OCT2 779 MATE1 415 OAT1 725 BSEP 550 OAT3 747 CYP3A5 136 P-gp 1741 BCRP 910 CYP1A2 2153 CYP2B6 926 CYP2C19 2057 OATP1B1 1079 OATP1B3 961 MATE2-K 77	MATE2-K 33 P-gp 2052 BCRP 697 MATE1 182 OAT3 391 OATP1B1 503 OATP1B3 435 OAT1 395 OCT2 434 CYP2C19 1119	CYP2C19 329 CYP2C8 198 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/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	no
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	no
CYP3A5 201	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	no
MATE2-K 77	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50 Page: 32 \| 50	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50 Page: 32 \| 50	no
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50 Page: 32 \| 50	no
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 49.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 49.0	no
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50 Page: 32 \| 50	no
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50 Page: 32 \| 50	no
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=50 Page: 32 \| 50	weak [IC50 22.6 uM]
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	yes
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	yes
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	yes
CYP2C8 1117	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	yes
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	yes
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=8 Page: 8.0	yes
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=33 Page: 33.0	yes
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=8 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=47 Page: 8 \| 47	yes	yes (co-administration study) Comment: Slightly decreased midazolam exposures (Cmax and AUCinf by 7% and 13%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=8 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=47 Page: 8 \| 47

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=7 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=17 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=40 Page: 7 \| 17 \| 27 \| 33 \| 40 \| 43	major	yes (pharmacogenomic study) Comment: Cmax and AUCinf of PM were significantly increased by 1.47-fold and 3.41-fold compared with NM Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=7 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=17 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=40 Page: 7 \| 17 \| 27 \| 33 \| 40 \| 43
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=27 Page: 27 \| 33	minor	yes (co-administration study) Comment: Itraconazole increased Cmax and AUC by 1.17-fold and 1.29-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=27 Page: 27 \| 33
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=7 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=17 Page: 7 \| 17 \| 27 \| 33 \| 45	minor	yes (co-administration study) Comment: Itraconazole increased Cmax and AUC by 1.17-fold and 1.29-fold Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=7 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=17 Page: 7 \| 17 \| 27 \| 33 \| 45
BCRP 697	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
MATE1 182	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
MATE2-K 33	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
OAT1 395	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
OAT3 391	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
OATP1B1 503	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
OATP1B3 435	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
OCT2 434	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=32 \| https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000ClinPharmR.pdf#page=49 Page: 32 \| 49	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2022/214998Orig1s000PharmR.pdf#page=78 Page: 78 \| 79

PubMed

Title	Date	PubMed

Patents

Sample Use Guides

In Vivo Use Guide

The recommended starting dose is 5 mg once daily without regard to food; allowable subsequent doses with titration are 2.5, 5, 10, or 15 mg once daily.

Route of Administration: Oral

In Vitro Use Guide

Treatment of mouse cardiac myofibrils with MYK-461 reduced ATPase activity in a dose-dependent manner [median inhibitory concentration (IC50) of 0.3 uM]. Maximal doses of MYK-461 (>10 uM) reduced the maximal ATPase rate by ~90%.

Name

Type

Language

MAVACAMTEN

Official Name

English

mavacamten [INN]

Preferred Name

English

Mavacamten [WHO-DD]

Common Name

English

CAMZYOS

Brand Name

English

SAR-439152

Code

English

2,4(1H,3H)-Pyrimidinedione, 3-(1-methylethyl)-6-[[(1S)-1-phenylethyl]amino]-

Systematic Name

English

3-(1-Methylethyl)-6-[[(1S)-1-phenylethyl]amino]-2,4(1H,3H)-pyrimidinedione

Systematic Name

English

MAVACAMTEN [USAN]

Common Name

English

MYK-461

Code

English

6-{[(1S)-1-phenylethyl]amino}-3-(propan-2-yl)pyrimidine-2,4(1H,3H)-dione

Systematic Name

English

Classification Tree Code System Code

FDA ORPHAN DRUG

515015