SARECYCLINE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C24H29N3O8
Molecular Weight	487.5024
Optical Activity	UNSPECIFIED
Defined Stereocenters	4 / 4
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

[H][C@@]12CC3=C(C(O)=CC=C3CN(C)OC)C(=O)C1=C(O)[C@]4(O)C(=O)C(C(N)=O)=C(O)[C@@H](N(C)C)[C@]4([H])C2

InChI

InChIKey=PQJQFLNBMSCUSH-SBAJWEJLSA-N

InChI=1S/C24H29N3O8/c1-26(2)18-13-8-11-7-12-10(9-27(3)35-4)5-6-14(28)16(12)19(29)15(11)21(31)24(13,34)22(32)17(20(18)30)23(25)33/h5-6,11,13,18,28,30-31,34H,7-9H2,1-4H3,(H2,25,33)/t11-,13-,18-,24-/m0/s1

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27139351
Curator's Comment: The description was created based on several sources, including https://clinicaltrials.gov/ct2/show/NCT02413346 | https://clinicaltrials.gov/ct2/show/NCT02651012 | https://clinicaltrials.gov/ct2/show/NCT02320149 | https://clinicaltrials.gov/ct2/show/NCT02322866 | https://www.drugbank.ca/drugs/DB12035 |

Sarecycline (SC1401, WC3035) is a novel, once-daily, tetracycline-derived compound being developed by Paratek Pharmaceuticals and Allergan (previously Actavis) for use in the treatment of acne and rosacea. In preclinical studies, Sarecycline possesses favorable anti-inflammatory activity, plus narrow-spectrum antibacterial activity relative to other tetracycline-derived molecules. Sarecycline has been used in Phase III clinical trials studying the treatment of Acne Vulgaris. The primary objective was to evaluate the efficacy and safety of oral Sarecycline 1.5 mg/kg per day compared to placebo in treating inflammatory acne lesions in subjects with moderate to severe acne. Sarecycline was statistically significantly superior to placebo with respect to primary efficacy endpoints. The most common adverse events (>2%) reported in the sarecycline group were nausea (3.2%), nasopharyngitis (2.8%), and headache (2.8%). The rate of discontinuation due to adverse events among sarecycline-treated patients in the two studies combined was 1.4%.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Bacterial 70S ribosome 179 Target ID: CHEMBL2363135 Sources: https://www.ncbi.nlm.nih.gov/pubmed/24002361	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Inflammatory lesions of non-nodular moderate to severe acne vulgaris 2 Sources: https://clinicaltrials.gov/ct2/show/NCT02322866	Curative		Approved 8429	SEYSARA Approved Use Seysara is specifically indicated for the treatment of inflammatory lesions of non-nodular moderate to severe acne vulgaris in patients 9 years of age and older. Launch Date 1.53826558E12

C_max

Value	Dose	Analyte	Population
1210 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
1590 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
1790 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
2570 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
2620 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
1700 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: FED
2480 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: FASTED
3820 ng/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
14000 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
20700 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
21800 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
32200 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
33800 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
31800 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: FED
43200 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: FASTED
48200 ng × h/mL OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
21.9 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	60 mg 1 times / day steady-state, oral dose: 60 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
20.7 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	100 mg 1 times / day steady-state, oral dose: 100 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN
20.9 h OTHER GOV https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	150 mg 1 times / day steady-state, oral dose: 150 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	SARECYCLINE plasma	Homo sapiens population: HEALTHY age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
1.5 mg/kg 1 times / day steady, oral (mean) Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p.93	unhealthy, 19.7 years (range: 9 to 45 years) n = 1300 Health Status: unhealthy Condition: acne vulgaris Age Group: 19.7 years (range: 9 to 45 years) Sex: M+F Population Size: 1300 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p.93	Disc. AE: Acne, Urticaria... AEs leading to discontinuation/dose reduction: Acne (3 patients) Urticaria (3 patients) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p.93
150 mg 1 times / day steady, oral Recommended Dose: 150 mg, 1 times / day Route: oral Route: steady Dose: 150 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	unhealthy, > 9 years Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf	Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf
1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209521s000lbl.pdf	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209521s000lbl.pdf	Other AEs: Nausea, Vulvovaginal mycotic infection... Other AEs: Nausea (3.1%) Vulvovaginal mycotic infection (0.8%) Vulvovaginal candidiasis (0.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209521s000lbl.pdf
1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17	Other AEs: Headache, Nasopharyngitis... Other AEs: Headache (3.1%) Nasopharyngitis (2.8%) Upper respiratory tract infection (1.6%) Blood creatine phosphokinase increased (1.2%) Diarrhea (1%) Oropharyngeal pain (1%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17

AEs

AE	Significance	Dose	Population
Acne	3 patients Disc. AE	1.5 mg/kg 1 times / day steady, oral (mean) Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p.93	unhealthy, 19.7 years (range: 9 to 45 years) n = 1300 Health Status: unhealthy Condition: acne vulgaris Age Group: 19.7 years (range: 9 to 45 years) Sex: M+F Population Size: 1300 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p.93
Urticaria	3 patients Disc. AE	1.5 mg/kg 1 times / day steady, oral (mean) Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p.93	unhealthy, 19.7 years (range: 9 to 45 years) n = 1300 Health Status: unhealthy Condition: acne vulgaris Age Group: 19.7 years (range: 9 to 45 years) Sex: M+F Population Size: 1300 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p.93
Vulvovaginal candidiasis	0.6%	1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209521s000lbl.pdf	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209521s000lbl.pdf
Vulvovaginal mycotic infection	0.8%	1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209521s000lbl.pdf	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209521s000lbl.pdf
Nausea	3.1%	1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209521s000lbl.pdf	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/209521s000lbl.pdf
Diarrhea	1%	1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17
Oropharyngeal pain	1%	1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17
Blood creatine phosphokinase increased	1.2%	1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17
Upper respiratory tract infection	1.6%	1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17
Nasopharyngitis	2.8%	1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17
Headache	3.1%	1.5 mg/kg 1 times / day steady, oral (mean) Recommended Dose: 1.5 mg/kg, 1 times / day Route: oral Route: steady Dose: 1.5 mg/kg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17	unhealthy, > 9 years n = 1064 Health Status: unhealthy Condition: acne vulgaris Age Group: > 9 years Population Size: 1064 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf Page: p. 17

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
	inhibitor 1767	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2A6 707 CYP2B6 810 CYP2C8 911 CYP2C19 1478 CYP2E1 882 CYP3A4/5 278 OATP1B1 788 OATP1B3 706 OCT2 647 OAT1 599 OAT3 642 BCRP 699 P-gp 1461	P-gp 1537 BCRP 561 OATP1B1 406 OATP1B3 350	CYP1A2 701 CYP2B6 547 CYP3A4/5 124

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/210496Orig1s000MultidisciplineR.pdf#page=46 Page: 58.0	no
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP3A4/5 335	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	yes [IC50 6.95 uM]	yes (co-administration study) Comment: In a drug interaction study conducted in healthy subjects, co-administration of a single dose of 150 mg sarecycline tablet caused a 26% increase in digoxin Cmax,ss while AUC0-tau,ss did not change compared to that when digoxin was dosed alone. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0

Drug as victim

Target	Modality	Activity
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=58 Page: 58.0	no

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/209521Orig1s000MultidisciplineR.pdf#page=37 Page: 37.0

Sourcing

Vendor/Aggregator	ID	URL
BLD Pharm	BD01114639	http://www.bldpharm.com/products/1035654-66-0.html
ChemShuttle	104918	http://www.chemshuttle.com/catalogsearch/result/?q=1035979-44-2&cat=
Chemieliva Pharmaceutical Co., Ltd	PBCM0036548
Compound Cloud	54681908
Compound Cloud	71296095
Matrix Scientific	145259	https://www.matrixscientific.com/145259.html
MuseChem	I012007	https://www.musechem.com/product/I012007.html
Smolecule	S542483	http://www.smolecule.com/products/s542483
THE BioTek	bt-281851	https://www.thebiotek.com/product/inhibitors/bt-281851
ZINC	ZINC000198637385	http://zinc15.docking.org/substances/ZINC000198637385
eMolecules	95740651

PubMed

Title	Date	PubMed
Looking for new preparations for antibacterial therapy. IV. New antimicrobial agents from the aminoglycoside, macrolide and tetracycline groups in clinical trials.	2015	27139351

Patents

Sample Use Guides

In Vivo Use Guide

1.5 mg/kg/day dose of oral sarecycline for duration of 12 week study

Route of Administration: Oral

In Vitro Use Guide

Unknown

Name

Type

Language

SARECYCLINE

Official Name

English

(4S,4aS,5aR,12aS)-4-(Dimethylamino)-3,10,12,12a-tetrahydroxy-7-[(methoxymethylamino)methyl]-1,11-dioxo-1,4,4a,5,5a,6,11,12a-octahydrotetracene-2-carboxamide

Systematic Name

English

Sarecycline [WHO-DD]

Common Name

English

SARECYCLINE [MI]

Common Name

English

(4S,4AS,5AR,12AS)-4-(DIMETHYLAMINO)-3,10,12,12A-TETRAHYDROXY-7-((METHOXY(METHYL)AMINO)METHYL)-1,11-DIOXO-1,4,4A,5,5A,6,11,12AOCTAHYDROTETRACENE-2-CARBOXAMIDE

Systematic Name

English

P-005672

Code

English

sarecycline [INN]

Common Name

English

SARECYCLINE [USAN]

Common Name

English

2-NAPHTHACENECARBOXAMIDE, 4-(DIMETHYLAMINO)-1,4,4A,5,5A,6,11,12A-OCTAHYDRO-3,10,12,12A-TETRAHYDROXY-7-((METHOXYMETHYLAMINO)METHYL)-1,11-DIOXO-, (4S,4AS,5AR,12AS)-

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C1595