TECOVIRIMAT MONOHYDRATE

Details

Stereochemistry	ACHIRAL
Molecular Formula	C19H15F3N2O3.H2O
Molecular Weight	394.3445
Optical Activity	UNSPECIFIED
Defined Stereocenters	6 / 6
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

O.[H][C@@]12C[C@]1([H])[C@@H]3C=C[C@H]2[C@@]4([H])C(=O)N(NC(=O)C5=CC=C(C=C5)C(F)(F)F)C(=O)[C@@]34[H]

InChI

InChIKey=QRHXYGPOQKLBJP-NPIFKJBVSA-N

InChI=1S/C19H15F3N2O3.H2O/c20-19(21,22)9-3-1-8(2-4-9)16(25)23-24-17(26)14-10-5-6-11(13-7-12(10)13)15(14)18(24)27;/h1-6,10-15H,7H2,(H,23,25);1H2/t10-,11+,12+,13-,14-,15+;

HIDE SMILES / InChI

Molecular Formula	H2O
Molecular Weight	18.0153
Charge	0
Count

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

Molecular Formula	C19H15F3N2O3
Molecular Weight	376.3292
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	6 / 6
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/16189015 | https://www.ncbi.nlm.nih.gov/pubmed/21994624

Tecovirimat (ST-246) is a low-molecular-weight compound (molecular weight = 376), that is potent (concentration that inhibited virus replication by 50% = 0.010 microM), selective (concentration of compound that inhibited cell viability by 50% = >40 microM), and active against multiple orthopoxviruses, including vaccinia, monkeypox, camelpox, cowpox, ectromelia (mousepox), and variola viruses. The antiviral activity is specific for orthopoxviruses and the compound does not inhibit the replication of other RNA- and DNA-containing viruses or inhibit cell proliferation at concentrations of compound that are antiviral. ST-246 targets vaccinia virus p37, a viral protein required for envelopment and secretion of extracellular forms of virus. The compound is orally bioavailable and protects multiple animal species from lethal orthopoxvirus challenge. rug substance and drug product processes have been developed and commercial scale batches have been produced using Good Manufacturing Processes (GMP). Human phase I clinical trials have shown that ST-246 is safe and well tolerated in healthy human volunteers. Based on the results of the clinical evaluation, once a day dosing should provide plasma drug exposure in the range predicted to be antiviral based on data from efficacy studies in animal models of orthopoxvirus disease.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
temporal expression: late 2 Target ID: 3707509.0 Gene Symbol: F13L Sources: https://www.ncbi.nlm.nih.gov/pubmed/16189015 \| https://www.ncbi.nlm.nih.gov/pubmed/25630650 \| https://www.ncbi.nlm.nih.gov/pubmed/22138484 \| https://www.ncbi.nlm.nih.gov/pubmed/19195323	Inhibitor 8297

Conditions

Condition	Modality	Targets	Highest Phase	Product
Human smallpox disease 2 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf	Curative		Approved 8429	TPOXX Approved Use TPOXX is an inhibitor of the orthopoxvirus VP37 envelope wrapping protein and is indicated for the treatment of human smallpox disease in adults and pediatric patients weighing at least 13 kg. Launch Date 2018

C_max

Value	Dose	Analyte	Population
1591 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29972742/	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	TECOVIRIMAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
2106 ng/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TECOVIRIMAT plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
2209 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29972742/	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TECOVIRIMAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED

AUC

Value	Dose	Analyte	Population
25876 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29972742/	600 mg single, oral dose: 600 mg route of administration: Oral experiment type: SINGLE co-administered:	TECOVIRIMAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED
28791 ng × h/mL DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TECOVIRIMAT plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
30632 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29972742/	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:	TECOVIRIMAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED

T_1/2

Value	Dose	Co-administered	Analyte	Population
20 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TECOVIRIMAT plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN
23 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/29972742/	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TECOVIRIMAT plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: FED

F_unbound

Value	Dose	Co-administered	Analyte	Population
20.5% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf	600 mg 2 times / day steady-state, oral dose: 600 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		TECOVIRIMAT plasma	Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
600 mg 2 times / day steady, oral Recommended Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf Page: 4	healthy, 18-79 years n = 359 Health Status: healthy Age Group: 18-79 years Sex: unknown Population Size: 359 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf Page: 4	Disc. AE: Abnormal EEG, Upset stomach... Other AEs: Headache, Nausea... AEs leading to discontinuation/dose reduction: Abnormal EEG (2%) Upset stomach (2%) Dry mouth (2%) Dysphoria (2%) Fever (2%) Palpable purpura (2%) Chills (2%) Facial swelling (2%) Gastrointestinal disorders (< 2%) Malaise (< 2%) Hematocrit decreased (< 2%) Hemoglobin decreased (< 2%) Heart rate increased (< 2%) Other AEs: Headache (12%) Nausea (5%) Abdominal pain (2%) Vomiting (2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf Page: 4
600 mg 2 times / day steady, oral Recommended Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf Page: 5	healthy, 18-79 years n = 359 Health Status: healthy Age Group: 18-79 years Sex: unknown Population Size: 359 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf Page: 5	Disc. AE: Arthralgia, Osteoarthritis... AEs leading to discontinuation/dose reduction: Arthralgia (< 2%) Osteoarthritis (< 2%) Psychiatric disorders (< 2%) Oropharyngeal pain (< 2%) Skin and subcutaneous tissue disorders (< 2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/208627s000lbl.pdf Page: 5
600 mg 2 times / day steady, oral Recommended Dose: 600 mg, 2 times / day Route: oral Route: steady Dose: 600 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000SumR.pdf Page: 14	healthy, 18-79 years n = 359 Health Status: healthy Age Group: 18-79 years Sex: unknown Population Size: 359 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000SumR.pdf Page: 14	Disc. AE: Abnormal EEG, Abdominal discomfort... AEs leading to discontinuation/dose reduction: Abnormal EEG (grade 1, < 2%) Abdominal discomfort (grade 1, < 2%) Dry mouth (grade 1, < 2%) Dysphoria (grade 1, < 2%) Disturbance in attention (grade 1, < 2%) Fever (grade 1, < 2%) Diarrhea (grade 2, < 2%) Nausea (grade 1, < 2%) Headache (grade 3, < 2%) Palpable purpura (grade 1, < 2%) Chills (grade 1, < 2%) Erythema (grade 1, < 2%) Pruritus (grade 1, < 2%) Facial swelling (grade 1, < 2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000SumR.pdf Page: 14
2000 mg single, oral Highest studied dose Dose: 2000 mg Route: oral Route: single Dose: 2000 mg Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346641/ Page: table 2	healthy, 30-33 years n = 7 Health Status: healthy Age Group: 30-33 years Sex: M+F Population Size: 7 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346641/ Page: table 2	Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346641/ Page: table 2
1000 mg single, oral Recommended Dose: 1000 mg Route: oral Route: single Dose: 1000 mg Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346641/ Page: table 2	healthy, 30-33 years n = 8 Health Status: healthy Age Group: 30-33 years Sex: M+F Population Size: 8 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346641/ Page: table 2	Other AEs: Neutropenia, Constipation... Other AEs: Neutropenia (12.5%) Constipation (12.5%) Headache (12.5%) Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346641/ Page: table 2
500 mg single, oral Recommended Dose: 500 mg Route: oral Route: single Dose: 500 mg Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346641/ Page: table 2	healthy, 30-33 years n = 8 Health Status: healthy Age Group: 30-33 years Sex: M+F Population Size: 8 Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346641/ Page: table 2	Other AEs: Feeling abnormal, Back pain... Other AEs: Feeling abnormal (12.5%) Back pain (12.5%) Headache (12.5%) Sources: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2346641/ Page: table 2

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1737 inhibitor 1587	inducer 389 substrate 1037 inhibitor 1767	substrate 1217 inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C8 911 CYP2C19 1478 CYP1A2 1524 CYP2A6 707 CYP2B6 810 CYP2E1 882 P-gp 1461 OATP1B1 788 OATP1B3 706 OAT1 599 OAT3 642 OCT2 647 BCRP 699	UGT1A1 418 UGT1A4 347 P-gp 1537 BCRP 561 CYP1A2 1054 CYP2B6 664 CYP2C8 693 CYP2C19 991 OATP1B1 406 OATP1B3 350 UGT1A3 422	CYP2B6 547 CYP3A 129

Drug as perpetrator

Target	Modality	Activity	Clinical evidence
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 70, 72	no
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 70, 72	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 70, 72	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 70, 72	no
CYP2E1 970	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 70, 72	no
CYP3A4 1925	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 70, 72	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 77	no
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 77	no
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 75	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 75	no
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 77	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 74	no
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 70, 72	no	no (co-administration study) Comment: flurbiprofen increased tecovirimat Cmax by 7% and AUC by 4% Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 70, 72
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 73	weak	no (co-administration study) Comment: tecovirimat induced mRNA expression of CYP2B6 at concentrations higher than 10 uM; bupropion decreased tecovirimat Cmax by 14% and AUC by 16%; tecovirimat is an inducer of CYP2B6/2C9/3A4 activities at 100 uM Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 73
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 73.0	weak	no (co-administration study) Comment: tecovirimat is an inducer of CYP2B6/2C9/3A4 activities at 100 uM Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 73.0
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 2, 3, 10, 24, 70	weak	yes (co-administration study) Comment: tecovirimat increased omeprazole Cmax by 86% and AUC by 72%; tecovirimat is not a TDI of CYP2C19 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 2, 3, 10, 24, 70
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 2, 3, 10, 24, 70	weak	yes (co-administration study) Comment: tecovirimat increased repaglinide Cmax by 27% and AUC by 29%; tecovirimat is not a TDI of CYP2C8 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 2, 3, 10, 24, 70
CYP3A 298	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 2, 3, 10, 24, 73	weak	yes (co-administration study) Comment: tecovirimat decreased midazolam Cmax by 39% and AUC by 32%; tecovirimat induced mRNA expression of CYP3A4 at concentrations higher than 10 uM; tecovirimat is an inducer of CYP2B6/2C9/3A4 activities at 100 uM Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 2, 3, 10, 24, 73
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 24, 75	yes [IC50 6.03 uM]

Drug as victim

Target	Modality	Activity	Clinical evidence
BCRP 561	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 14.0	no
CYP1A2 1054	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 15, 67	no
CYP2B6 664	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 15, 67	no
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 15, 67	no
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 15, 67	no
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 15, 67	no
CYP2D6 1217	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 15, 67	no
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 15, 67	no
OATP1B1 406	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 15, 75	no
OATP1B3 350	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 15, 75	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 14.0	no
UGT1A3 422	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 56.0	yes
UGT1A1 418	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 10, 24, 68	yes	yes (co-administration study) Comment: tecovirimat exposures can be increased or decreased by the use of UGT1A1/4 inhibitor or inducers, respectively Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 10, 24, 68
UGT1A4 347	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 10, 24, 68	yes	yes (co-administration study) Comment: tecovirimat exposures can be increased or decreased by the use of UGT1A1/4 inhibitor or inducers, respectively Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000ClinPharmR.pdf Page: 10, 24, 68

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2018/208627Orig1s000PharmR.pdf Page: 94.0

Sourcing

Vendor/Aggregator	ID	URL
AN PharmaTech	AN-27268
Ambinter	Amb24076326	http://www.ambinter.com/reference/24076326
ApexBio Technology	B4829	http://www.apexbt.com/tecovirimat.html
BOC Sciences	816458-31-8
BioCrick	BCC5518	http://www.biocrick.com/Tecovirimat-BCC5518.html
Chem Scene	CS-3464
ChemShuttle	139092	http://www.chemshuttle.com/catalogsearch/result/?q=869572-92-9&cat=
Chemieliva Pharmaceutical Co., Ltd	PBCM1443390
Excenen	EX-A4340	https://www.excenen.com/searchresultlist.php?id=EX-A4340
Lab Network	LN01342004
Lan Pharmatech	LAN-B47248
Lan Pharmatech	LQT-B47339
MedChem Express	HY-14805
MolPort	MolPort-047-769-294	https://www.molport.com/shop/molecule-link/MolPort-047-769-294
Norris Pharm	NSZB-A271256
OChem	27601	http://www.ocheminc.com/index.php?act=psearch&pid=458T318
Race Chemical	RV022513667
Selleck Chemicals	S3380	http://www.selleckchem.com/products/tecovirimat.html
ZINC	ZINC000035323125	http://zinc15.docking.org/substances/ZINC000035323125
eMolecules	82744279
mcule	MCULE-1536691472

PubMed

Title	Date	PubMed
An orally bioavailable antipoxvirus compound (ST-246) inhibits extracellular virus formation and protects mice from lethal orthopoxvirus Challenge.	2005 Oct	16189015
Tricyclononene carboxamide derivatives as novel anti-HIV-1 agents.	2010 Sep	20598780

Patents

Sample Use Guides

In Vivo Use Guide

Phase 2, double-blind, randomized, placebo-controlled, multicenter trial was conducted to assess the safety, tolerability, and pharmacokinetics (PK) of tecovirimat (ST-246) when administered as a single daily oral dose (400 mg or 600 mg) for 14 days in fed adult volunteers.

Route of Administration: Oral

In Vitro Use Guide

BSC-40 cells were infected with 2 PFU/cell of vaccinia virus and incubated in the presence and absence of 5 uM tecovirimat (ST-246) . At selected times postinfection, extracellular virus in the medium and cell associated virus were quantified by plaque assay. The results show that ST-246 reduced extracellular virus titers by approximately 10 fold at 24 h postinfection, while having little effect on the level of intracellular virus titers relative to untreated controls. These results suggest that ST-246 inhibits extracellular virus formation.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 08:38:56 GMT 2023` Edited by `admin` on `Sat Dec 16 08:38:56 GMT 2023`
Record UNII	SB96YO2BR8
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TECOVIRIMAT MONOHYDRATE

Common Name

English

BENZAMIDE, N-((3AR,4R,4AR,5AS,6S,6AS)-3,3A,4,4A,5,5A,6,6A-OCTAHYDRO-1,3-DIOXO-4,6-ETHENOCYCLOPROP(F)ISOINDOL-2(1H)-YL)-4-(TRIFLUOROMETHYL)-, HYDRATE (1:1), REL-

Systematic Name

English

TPOXX

Brand Name

English

ST-246 MONOHYDRATE

Code

English

Tecovirimat monohydrate [WHO-DD]

Common Name

English

TECOVIRIMAT MONOHYDRATE [MI]

Common Name

English

Code System Code Type Description

FDA UNII

SB96YO2BR8