TICAGRELOR MONOHYDRATE

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C23H28F2N6O4S.H2O
Molecular Weight	540.583
Optical Activity	UNSPECIFIED
Defined Stereocenters	6 / 6
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.CCCSC1=NC2=C(N=NN2[C@@H]3C[C@H](OCCO)[C@@H](O)[C@H]3O)C(N[C@@H]4C[C@H]4C5=CC(F)=C(F)C=C5)=N1

InChI

InChIKey=LXLCTRJKFYBHRD-VQNGXBDNSA-N

InChI=1S/C23H28F2N6O4S.H2O/c1-2-7-36-23-27-21(26-15-9-12(15)11-3-4-13(24)14(25)8-11)18-22(28-23)31(30-29-18)16-10-17(35-6-5-32)20(34)19(16)33;/h3-4,8,12,15-17,19-20,32-34H,2,5-7,9-10H2,1H3,(H,26,27,28);1H2/t12-,15+,16+,17-,19-,20+;/m0./s1

HIDE SMILES / InChI

Description
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022433s015lbl.pdf
Curator's Comment: description was created based on several sources, including http://www.ema.europa.eu/docs/en_GB/document_library/PIP_decision/WC500123240.pdf; http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Summary_for_the_public/human/002303/WC500100562.pdf; https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf

Ticagrelor (known trade names Brilinta, Brilique and Possia) is a P2Y12 platelet inhibitor. Brilinta has been approved by the US Food and Drug administration (FDA) in 2011 and is indicated to reduce the rate of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome (ACS) or a history of myocardial infarction. Brilinta also reduces the rate of stent thrombosis in patients who have been stented for treatment of ACS. Ticagrelor and its major metabolite reversibly interact with the platelet P2Y12 ADP-receptor to prevent signal transduction and platelet activation. Ticagrelor and its active metabolite are approximately equipotent. In vitro metabolism studies demonstrate that ticagrelor and its major active metabolite are weak inhibitors of CYP3A4, potential activators of CYP3A5 and inhibitors of the P-gp transporter. Most common adverse reactions are bleeding 12% and dyspnea 14%.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Purinergic receptor P2Y12 23 Target ID: CHEMBL2001 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022433s015lbl.pdf	Antagonist 2849

Conditions

Condition	Modality	Targets	Highest Phase	Product
Acute coronary syndrome 33 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022433s015lbl.pdf	Secondary		Approved 8583	BRILINTA Approved Use Indicated to reduce the rate of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI). For at least the first 12 months following ACS, it is superior to clopidogrel. Reduces the rate of stent thrombosis in patients who have been stented for treatment of ACS. Launch Date 2011
Myocardial infarction 125 Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022433s015lbl.pdf	Secondary		Approved 8583	BRILINTA Approved Use Indicated to reduce the rate of cardiovascular death, myocardial infarction, and stroke in patients with acute coronary syndrome (ACS) or a history of myocardial infarction (MI). For at least the first 12 months following ACS, it is superior to clopidogrel. Reduces the rate of stent thrombosis in patients who have been stented for treatment of ACS. Launch Date 2011

C_max

Value	Dose	Analyte	Population
1208 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01898442	270 mg single, oral dose: 270 mg route of administration: oral experiment type: single co-administered:	TICAGRELOR plasma	Homo sapiens
1208 ng/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01898442	360 mg single, oral dose: 360 mg route of administration: oral experiment type: single co-administered:	TICAGRELOR plasma	Homo sapiens
1583 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20642549/	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TICAGRELOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
12379 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01898442	270 mg single, oral dose: 270 mg route of administration: oral experiment type: single co-administered:	TICAGRELOR plasma	Homo sapiens
12381 ng*h/mL Clinical Trial https://clinicaltrials.gov/ct2/show/NCT01898442	360 mg single, oral dose: 360 mg route of administration: oral experiment type: single co-administered:	TICAGRELOR plasma	Homo sapiens
10160 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/20642549/	200 mg 2 times / day multiple, oral dose: 200 mg route of administration: Oral experiment type: MULTIPLE co-administered:	TICAGRELOR plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Co-administered	Analyte	Population
7 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022433s028lbl.pdf	90 mg single, oral dose: 90 mg route of administration: Oral experiment type: SINGLE co-administered:		TICAGRELOR plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
1% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/022433s028lbl.pdf	90 mg single, oral dose: 90 mg route of administration: Oral experiment type: SINGLE co-administered:		TICAGRELOR plasma	Homo sapiens population: UNKNOWN age: ADULT sex: FEMALE / MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj	healthy Health Status: healthy Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj	DLT: Gastrointestinal disorder NOS, Sinus arrest... Dose limiting toxicities: Gastrointestinal disorder NOS (50%) Sinus arrest (serious, 16.7%) High grade atrioventricular block (serious, 16.7%) Ventricular escape rhythm (serious, 16.7%) Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj
900 mg single, oral MTD Dose: 900 mg Route: oral Route: single Dose: 900 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj	healthy Health Status: healthy Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj	Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj
90 mg 2 times / day multiple, oral Recommended Dose: 90 mg, 2 times / day Route: oral Route: multiple Dose: 90 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf	unhealthy Health Status: unhealthy Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf	Disc. AE: Dyspnea... AEs leading to discontinuation/dose reduction: Dyspnea (0.9%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf
90 mg 2 times / day multiple, oral Recommended Dose: 90 mg, 2 times / day Route: oral Route: multiple Dose: 90 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf	Disc. AE: Bleeding... AEs leading to discontinuation/dose reduction: Bleeding (grade 3-5) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf

AEs

AE	Significance	Dose	Population
Gastrointestinal disorder NOS	50% DLT	1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj	healthy Health Status: healthy Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj
High grade atrioventricular block	serious, 16.7% DLT	1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj	healthy Health Status: healthy Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj
Sinus arrest	serious, 16.7% DLT	1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj	healthy Health Status: healthy Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj
Ventricular escape rhythm	serious, 16.7% DLT	1260 mg single, oral Highest studied dose Dose: 1260 mg Route: oral Route: single Dose: 1260 mg Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj	healthy Health Status: healthy Sources: https://pubmed.ncbi.nlm.nih.gov/24040849 https://www.google.ru/url?sa=t&rct=j&q=&esrc=s&source=web&cd=&ved=2ahUKEwji45rs27fuAhVmiYsKHW3hA2MQFjAGegQICBAC&url=https%3A%2F%2Fwww.tga.gov.au%2Ffile%2F797%2Fdownload&usg=AOvVaw3STEHV1bh8A3ZobpKVV1Gj
Dyspnea	0.9% Disc. AE	90 mg 2 times / day multiple, oral Recommended Dose: 90 mg, 2 times / day Route: oral Route: multiple Dose: 90 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf	unhealthy Health Status: unhealthy Sex: M+F Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf
Bleeding	grade 3-5 Disc. AE	90 mg 2 times / day multiple, oral Recommended Dose: 90 mg, 2 times / day Route: oral Route: multiple Dose: 90 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/022433s020lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252 inducer 1087	substrate 1193 inhibitor 2438 inducer 440	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
Cav1.2 58 Nav1.5 116 Kv1.5 27 Cav3.2 12 CYP3A5 136 CYP1A2 2153 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 CYP2E1 1060 P-gp 1741 OAT3 747 OAT1 725 UGT1A1 246 L-type Ca channels 9	CYP3A5 446 CYP1A2 1197 CYP2A6 626 CYP2B6 776 CYP2C19 1119 P-gp 2052	CYP1A1 151 CYP1A2 832 CYP2B6 669

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=13 Page: 13.0	likely
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=13 Page: 13.0	likely	AR-C124910XX 3
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13	likely
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13	likely	AR-C124910XX 3
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11	moderate [IC50 10.5 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11	moderate [IC50 11.7 uM]	AR-C124910XX 3
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11	moderate [IC50 26.7 uM]
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=127 Page: 9-11, (PMDA) 127	moderate [IC50 33 uM]	AR-C124910XX 3
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=127 Page: 9-11, (PMDA) 127	moderate [IC50 43 uM]	AR-C124910XX 3
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11	moderate [IC50 6.9 uM]	AR-C124910XX 3	no (co-administration study) Comment: Human liver microsomes, dicrofenac (substrate); Co-administration of ticagrelor (180 mg BID x 9 days) did not alter the systemic exposure of tolbutamide (500 mg QD on Day 5, CYP2C9 substrate) (GM ratio of AUCinf and Cmax were 103%, 110%, while 4-OH tolbutamide AUCinf GM ratio and Cmax GM ratio were 94% and 90%). Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11
CYP3A5 201	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=130 Page: 9-12, (PMDA) 130	moderate [IC50 7.6 uM]	AR-C124910XX 3
CYP3A5 201	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=60, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=66, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=130 Page: 9-12, 60-61, 66-67, (PMDA) 130	moderate [IC50 8.2 uM]		yes (co-administration study) Comment: Human liver microsomes, midazolam (4-hydroxylation, substrate), no time-dependent inhibition; Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day1, 180 mg BID on Days 2-7) significantly increased simvastatin (80 mg on Day 5, CYP3A4/5 substrate) AUCinf by 56% and Cmax 81%, and simvastatin acid AUCinf by 52% and Cmax by 64%. Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day1, 180 mg BID on Days 2-7) significantly reduced oral midazolam (7.5 mg AM on Days 1 & 7) AUCinf by 10%, and 4’-OH-midazolam by 42%. Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day 1, 180 mg BID on Days 2-7) does not alter the systemic exposure of IV midazolam (2.5 mg IV over 2 min AM on Days 1 & 7) and significantly reduced 4’-OH- midazolam systemic exposure by ~ 23%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=60, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=66, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=130 Page: 9-12, 60-61, 66-67, (PMDA) 130
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=127 Page: 9-12, (PMDA) 127	no [IC50 40 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11	no [IC50 >50 uM]
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11	no [IC50 >50 uM]	AR-C124910XX 3
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11	no [IC50 >50 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=127 Page: 9-11, (PMDA) 127	no [IC50 >50 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11	no [IC50 >50 uM]	AR-C124910XX 3
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, Page: 9-11	no [IC50 >50 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=62, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=64, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=66, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=124, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=130 Page: 9-12, 62-63, 64-65, 66-67 (PMDA) 124-125, 130	no [IC50 >50 uM]		weak (co-administration study) Comment: Human liver microsomes, midazolam (1-hydroxylation, substrate), midazolam 1-hydroxylation was activated in the presence of Cyt-b5 by 144.9% (CYP3A4 (cDNA expressed enzyme):Cyp-b5 = 1: 3 + 5.56 mcM ticagrelor), no time-dependent inhibition; Inhibited testosterone intrinsic clearance (IC50 = 23 mcM, pooled human liver microsomes (33 male and female donors); Co-administration of ticagrelor (270 mg AM + 90 mg PM on Day 1, 90 mg BID on Days 2-7) significantly increased atorvastatin (80 mg QD on Day 5) AUCinf 36% and Cmax 23%, atorvastatin lactone AUCinf 32% and Cmax 39%, s 2-OH atorvastatin AUCinf 33% and Cmax 13%, and 4-OH atorvastatin AUCinf 67% and Cmax 55%. Co-administration of ticagrelor (90 mg BID x 21 days) significantly increased ethinyl estradiol AUCinf, Cmax, and Cmin by 20%, 30.6%, and 20.2%, respectively. Co-administration of ticagrelor does not alter the systemic exposure of levonorgestrel. Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day1, 180 mg BID on Days 2-7) significantly reduced oral midazolam (7.5 mg AM on Days 1 & 7) AUCinf by 10%, but did not alter 1’-OH- midazolam AUC. Co-administration of ticagrelor (270 mg AM + 180 mg PM on Day 1, 180 mg BID on Days 2-7) did not alter the systemic exposure of IV midazolam (2.5 mg IV over 2 min AM on Days 1 & 7) and 1’-OH-midazolam. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=62, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=64, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=66, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=124, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=130 Page: 9-12, 62-63, 64-65, 66-67 (PMDA) 124-125, 130
CYP1A1 272	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=14, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=139 Page: 14, (PMDA) 139	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13	no	AR-C124910XX 3
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=12 Page: 12-13	no	AR-C124910XX 3
CYP3A4 2633	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=9, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=130 Page: 9-12, (PMDA) 130	no	AR-C124910XX 3
OAT1 730	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161	no
OAT1 730	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161	no	AR-C133913XX 3
OAT3 749	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161	strong [Ki 13.4 uM]	AR-C133913XX 3
OAT3 749	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161	strong [Ki 16.3 uM]	AR-C124910XX 3
OAT3 749	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161	strong [Ki 4.9 uM]
OAT1 730	inhibitor 4027 Sources: https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=160 Page: (PMDA) 160-161	strong	AR-C124910XX 3
L-type Ca channels 9	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=116 Page: 116.0	weak
L-type Ca channels 9	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=116 Page: 116.0	weak	AR-C124910XX 3
UGT1A1 303	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 26, 117	yes [IC50 0.759 uM]	AR-C124910XX 3
UGT1A1 303	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 26, 117	yes [IC50 1 uM]
Kv1.5 42	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0	yes [IC50 10 uM]
Kv1.5 42	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0	yes [IC50 16.9 uM]	AR-C124910XX 3
Cav3.2 12	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0	yes [IC50 19.2 uM]
Cav3.2 12	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0	yes [IC50 19.9 uM]	AR-C124910XX 3
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=58, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=157 Page: 4-5, 58-59 (PMDA) 157	yes [IC50 7.8 uM]		yes (co-administration study) Comment: MDR1-MDCK monolayer, H3-digoxin (5 mcM) as a substrate, Flux ratio = 19.5 (digoxin only), 3.1 (digoxin + 10 mcM Ticagrelor); Co-administration of ticagrelor (400 mg QD, Days 1-16) significantly increased digoxin (0.25 mg BID on Day 6, 0.25 mg QD on Days 7-14, P-gp substrate) AUC0-72, Css,max, and Css, min by 28%, 75% and 31%, respectively. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=4, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=58, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=157 Page: 4-5, 58-59 (PMDA) 157
P-gp 1932	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=4, https://www.pmda.go.jp/drugs/2016/P20161026001/670227000_22800AMX00680_I100_1.pdf#page=157 Page: 4-5, (PMDA) 157	yes [IC50 9.9 uM]	AR-C124910XX 3

Drug as victim

Target	Modality	Activity	Metabolite	Clinical evidence
CYP3A4 1946	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=123, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=6, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=43 Page: 123, (ClinPharm) 5-6, 43-44, 45-47, 47-49	major [Km 11 uM]		yes (co-administration study) Comment: Human liver microsomes (determination of CYPs) and human cDNA expressed emzymes (Km for AR-C124910XX formation), Km (AR-C124910XX, human liver microsomes) = 27 mcM; Km (AR-C133913XX formation) = 41 mcM; Co-administration of ketoconazole (200 mg BID for 10 days, CYP3A4 inhibitor) significantly increased ticagrelor (90 mg QD on Day 4) AUCinf by 7.32 fold and Cmax by 2.35 fold, and decreased AR-C124910XX AUCinf by 56% and Cmax by 89%. Co-administration of diltiazem (240 mg QD x 14 days, moderate CYP3A4 inhibitor) significantly increased ticagrelor (90 mg QD on Day 8) AUCinf by 2.74 fold and Cmax by 1.69, and decreased AR-C124910XX AUCinf by 13% and Cmax by 38%. Co-administration of rifampin (600 mg QD Days 4-17, strong CYP3A4/P-gp inducer) significantly decreased ticagrelor (180 mg QD Days 1 & 15) AUCinf by 86% and Cmax by 73%, and decreased AR-C124910XX AUCinf by 46% and did not affect Cmax. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=123, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=6, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=43 Page: 123, (ClinPharm) 5-6, 43-44, 45-47, 47-49
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=6 Page: 6.0	no
CYP2A6 626	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=6 Page: 6.0	no
CYP2B6 776	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=6 Page: 6.0	no
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=6 Page: 6.0	no
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=6 Page: 6.0	no
CYP2D6 1388	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=6 Page: 6.0	no
CYP3A5 446	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=123, https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=6 Page: 123, (ClinPharm) 5-6	yes [Km 5.36 uM]
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=4 Page: 4.0	yes
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000ClinPharmR.pdf#page=4 Page: 4.0	yes	AR-C124910XX 3

Tox targets

Target	Modality	Metabolite
Cav1.2 63	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0
Cav1.2 63	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0	AR-C124910XX 3
Nav1.5 119	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0
Nav1.5 119	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=117 Page: 117.0	AR-C124910XX 3
hERG 2263	inhibitor 2237 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022433Orig1s000PharmR.pdf#page=119 Page: 119.0

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:68558	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:68558
ChemicalBook	CB51509134	https://www.chemicalbook.com/ChemicalProductProperty_EN_CB51509134
eMolecules	36756307	https://www.emolecules.com/cgi-bin/more?vid=36756307
MolPort	MolPort-023-329-971	https://www.molport.com/shop/molecule-link/MolPort-023-329-971
Selleck Chemicals	ticagrelor	http://www.selleckchem.com/products/ticagrelor.html
ZINC	ZINC000028957444	http://zinc15.docking.org/substances/ZINC000028957444

PubMed

Title	Date	PubMed
State of the art of new P2Y12 antagonists.	2010-10	20177818
Balancing the benefits and risks of antiplatelet agents in patients with non-ST-segment elevated acute coronary syndromes and undergoing percutaneous coronary intervention.	2010-08	20111983
The case for routine genotyping in dual-antiplatelet therapy.	2010-07-06	20471193
PLATO study of ticagrelor versus clopidogrel in patients with high-risk acute coronary syndromes.	2010-07	20432073
Antiplatelet therapy in percutaneous coronary intervention: recent advances in oral antiplatelet agents.	2010-07	20421791
Examining biology and pharmacology-based hypotheses in the PLATO trial.	2010-07	20414795
The role of antiplatelet therapy in the secondary prevention of coronary artery disease.	2010-07	20386440
The year in interventional cardiology.	2010-05-18	20466207
Forecasting drug utilization and expenditure in a metropolitan health region.	2010-05-17	20478043
Antiplatelet drugs--do we need new options? With a reappraisal of direct thromboxane inhibitors.	2010-05-07	20426498
Pharmacokinetics, pharmacodynamics, tolerability and safety of single ascending doses of ticagrelor, a reversibly binding oral P2Y(12) receptor antagonist, in healthy subjects.	2010-05	20091161
Advances in antiplatelet treatment for acute coronary syndromes.	2010-05	19910292
Stabilizing role of platelet P2Y(12) receptors in shear-dependent thrombus formation on ruptured plaques.	2010-04-12	20405028
Changes in inflammatory biomarkers in patients treated with ticagrelor or clopidogrel.	2010-04	20394040
[Update: oral platelet inhibitors in cardiology].	2010-04	20333345
Antiplatelet therapy prasugrel: a novel platelet ADP P2Y12 receptor antagonist.	2010-04	20299391
The PLATO trial: do you believe in magic?	2010-04	20007979
Role of ticagrelor in clopidogrel nonresponders: resistance is futile?	2010-03-16	20194888
Response to ticagrelor in clopidogrel nonresponders and responders and effect of switching therapies: the RESPOND study.	2010-03-16	20194878
Management of antiplatelet therapy during acute percutaneous coronary intervention: new strategies and therapeutics.	2010-03	20372759
Advances in antiplatelet therapy for stroke prevention: the new P2Y12 antagonists.	2010-03	20210760
Efficacy and safety of ticagrelor: a reversible P2Y12 receptor antagonist.	2010-03	20124464
The novel P2Y 12 antagonist AZD6140 rapidly and reversibly reduces platelet activation in diabetic rats.	2010-03	19846210
Pharmacokinetic, pharmacodynamic and clinical profile of novel antiplatelet drugs targeting vascular diseases.	2010-02-01	20050853
Mechanism of action and clinical development of ticagrelor, a novel platelet ADP P2Y12 receptor antagonist.	2010-02	20136601
The year in cardiothoracic and vascular anesthesia: selected highlights from 2009.	2010-02	20123237
Limitations of current therapies to prevent thrombosis: a need for novel strategies.	2010-02	20094648
New drugs for the treatment of coronary artery syndromes: otamixaban and ticagrelor.	2010-02	20088750
The TRITON versus PLATO trials: differences beyond platelet inhibition.	2010-02	20024505
Ticagrelor in ACS: redefining a new standard of care?	2010-01-23	20079529
Comparison of ticagrelor with clopidogrel in patients with a planned invasive strategy for acute coronary syndromes (PLATO): a randomised double-blind study.	2010-01-23	20079528
[Update on new antithrombotic treatments].	2010-01-20	20170027
Ticagrelor, a new antiplatelet agent, for prevention of ischemic events in patients with coronary artery disease.	2010-01	20425218
Recent advances in cardiology.	2010-01	20014984
[Ticagrelor versus clopidogrel in patients with acute coronary syndromes: results of the PLATO study].	2010	20144161
Randomized double-blind assessment of the ONSET and OFFSET of the antiplatelet effects of ticagrelor versus clopidogrel in patients with stable coronary artery disease: the ONSET/OFFSET study.	2009-12-22	19923168
ACP Journal Club. Ticagrelor was more effective than clopidogrel, with no increase in major bleeding in acute coronary syndromes.	2009-12-15	20008753
Ticagrelor versus clopidogrel in acute coronary syndromes.	2009-12-10	20050198
Ticagrelor versus clopidogrel in acute coronary syndromes.	2009-12-10	20050197
Ticagrelor versus clopidogrel in acute coronary syndromes.	2009-12-10	20050196
Ticagrelor versus clopidogrel in acute coronary syndromes.	2009-12-10	20007565
Ticagrelor--a new platelet aggregation inhibitor in patients with acute coronary syndromes. An improvement of other inhibitors?	2009-12	19946242
Antiplatelet therapy: Ticagrelor in ACS-what does PLATO teach us?	2009-12	19935680
New antiplatelet agents: why they are needed.	2009-12	19892299
Oral antiplatelet therapy for acute and chronic management of NSTE ACS: residual ischemic risk and opportunities for improvement.	2009-12	19890703
Strategy for the treatment of clopidogrel low responsiveness in diabetes mellitus and stent implantation.	2009-11	19997540
HOTLINE I, PLATO favours ticagrelor over clopidogrel in ACS.	2009-11	19891080
P2Y12 inhibitors: thienopyridines and direct oral inhibitors.	2009-11	19882081
Update on antiplatelet therapy in acute coronary syndromes: what do new drugs bring into clinical practice?	2009	20000883
Aspirin and clopidogrel hyporesponsiveness and nonresponsiveness in patients with coronary artery stenting.	2009	19997577

Patents

Sample Use Guides

In Vivo Use Guide

Initiate treatment with 180 mg (two 90 mg tablets) oral loading dose. Continue treatment with 90 mg twice daily.

Route of Administration: Oral

In Vitro Use Guide

In human liver microsomes, ticagrelor inhibited midazolam 4-hydroxylation with an IC50 of 8.2 uM. Evaluated in fresh human hepatocytes at concentration up to 20 uM, ticagrelor was not an inducer of CYP1A2 or CYP3A4.

Name

Type

Language

TICAGRELOR HYDRATE

Preferred Name

English

TICAGRELOR MONOHYDRATE

Common Name

English

1,2-CYCLOPENTANEDIOL, 3-(7-(((1R,2S)-2-(3,4-DIFLUOROPHENYL)CYCLOPROPYL)AMINO)-5-(PROPYLTHIO)-3H-1,2,3-TRIAZOLO(4,5-D)PYRIMIDIN-3-YL)-5-(2-HYDROXYETHOXY)-, HYDRATE (1:1), (1S,2S,3R,5S)-

Systematic Name

English

TICAGRELOR MONOHYDRATE, (-)-

Common Name

English

Code System Code Type Description

PUBCHEM

77107968

Created by admin on Mon Mar 31 23:20:06 GMT 2025 , Edited by admin on Mon Mar 31 23:20:06 GMT 2025

PRIMARY

FDA UNII

0UZ317Q903

Created by admin on Mon Mar 31 23:20:06 GMT 2025 , Edited by admin on Mon Mar 31 23:20:06 GMT 2025

PRIMARY

CAS

377093-13-5

Created by admin on Mon Mar 31 23:20:06 GMT 2025 , Edited by admin on Mon Mar 31 23:20:06 GMT 2025

NON-SPECIFIC STOICHIOMETRY

CAS

1648912-09-7

Created by admin on Mon Mar 31 23:20:06 GMT 2025 , Edited by admin on Mon Mar 31 23:20:06 GMT 2025

PRIMARY

PARENT (SALT/SOLVATE)


					GLH0314RVC

TICAGRELOR

SUBSTANCE RECORD


					0UZ317Q903

TICAGRELOR MONOHYDRATE

Details

SMILES

InChI

Originator

Approval Year

Targets

Conditions

Approved Use

Launch Date

Approved Use

Launch Date

Cmax

AUC

T1/2

Funbound

Doses

AEs

Overview

OverviewOther

Drug as perpetrator​

Drug as victim

Tox targets

Sourcing

PubMed

Patents

Sample Use Guides

C_max

T_1/2

F_unbound

Drug as perpetrator