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Details

Stereochemistry ACHIRAL
Molecular Formula C19H15F3N2O3.H2O
Molecular Weight 394.3452
Optical Activity UNSPECIFIED
Defined Stereocenters 6 / 6
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of TECOVIRIMAT MONOHYDRATE

SMILES

c1cc(ccc1C(=O)NN2C(=O)[C@@]3([H])[C@@]4([H])C=C[C@]([H])([C@]5([H])C[C@]45[H])[C@@]3([H])C2=O)C(F)(F)F.O

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
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

Curator's Comment:: Tecovirimat (ST-246) is CNS penetrant in animals. No human data available.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
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

1.53135363E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1591 ng/mL
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
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
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

AUC

ValueDoseCo-administeredAnalytePopulation
25876 ng × h/mL
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
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
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
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
20 h
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
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
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
20.5%
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

Doses

DosePopulationAdverse 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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: 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: 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: Page: 5
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: 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: 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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: 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: Page: 14
2000 mg single, oral
Highest studied dose
Dose: 2000 mg
Route: oral
Route: single
Dose: 2000 mg
Sources: Page: table 2
healthy, 30-33 years
n = 7
Health Status: healthy
Age Group: 30-33 years
Sex: M+F
Population Size: 7
Sources: Page: table 2
1000 mg single, oral
Recommended
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources: Page: table 2
healthy, 30-33 years
n = 8
Health Status: healthy
Age Group: 30-33 years
Sex: M+F
Population Size: 8
Sources: Page: table 2
Other AEs: Neutropenia, Constipation...
Other AEs:
Neutropenia (12.5%)
Constipation (12.5%)
Headache (12.5%)
Sources: Page: table 2
500 mg single, oral
Recommended
Dose: 500 mg
Route: oral
Route: single
Dose: 500 mg
Sources: Page: table 2
healthy, 30-33 years
n = 8
Health Status: healthy
Age Group: 30-33 years
Sex: M+F
Population Size: 8
Sources: Page: table 2
Other AEs: Feeling abnormal, Back pain...
Other AEs:
Feeling abnormal (12.5%)
Back pain (12.5%)
Headache (12.5%)
Sources: Page: table 2
AEs

AEs

AESignificanceDosePopulation
Headache 12%
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Abdominal pain 2%
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Vomiting 2%
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Abnormal EEG 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Chills 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Dry mouth 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Dysphoria 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Facial swelling 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Fever 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Palpable purpura 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Upset stomach 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Nausea 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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Gastrointestinal disorders < 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Heart rate increased < 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Hematocrit decreased < 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Hemoglobin decreased < 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Malaise < 2%
Disc. AE
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: Page: 4
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 4
Arthralgia < 2%
Disc. AE
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: Page: 5
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 5
Oropharyngeal pain < 2%
Disc. AE
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: Page: 5
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 5
Osteoarthritis < 2%
Disc. AE
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: Page: 5
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 5
Psychiatric disorders < 2%
Disc. AE
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: Page: 5
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 5
Skin and subcutaneous tissue disorders < 2%
Disc. AE
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: Page: 5
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 5
Abdominal discomfort grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Abnormal EEG grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Chills grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Disturbance in attention grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Dry mouth grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Dysphoria grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Erythema grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Facial swelling grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Fever grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Nausea grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Palpable purpura grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Pruritus grade 1, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Diarrhea grade 2, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Headache grade 3, < 2%
Disc. AE
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: Page: 14
healthy, 18-79 years
n = 359
Health Status: healthy
Age Group: 18-79 years
Sex: unknown
Population Size: 359
Sources: Page: 14
Constipation 12.5%
1000 mg single, oral
Recommended
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources: Page: table 2
healthy, 30-33 years
n = 8
Health Status: healthy
Age Group: 30-33 years
Sex: M+F
Population Size: 8
Sources: Page: table 2
Headache 12.5%
1000 mg single, oral
Recommended
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources: Page: table 2
healthy, 30-33 years
n = 8
Health Status: healthy
Age Group: 30-33 years
Sex: M+F
Population Size: 8
Sources: Page: table 2
Neutropenia 12.5%
1000 mg single, oral
Recommended
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources: Page: table 2
healthy, 30-33 years
n = 8
Health Status: healthy
Age Group: 30-33 years
Sex: M+F
Population Size: 8
Sources: Page: table 2
Back pain 12.5%
500 mg single, oral
Recommended
Dose: 500 mg
Route: oral
Route: single
Dose: 500 mg
Sources: Page: table 2
healthy, 30-33 years
n = 8
Health Status: healthy
Age Group: 30-33 years
Sex: M+F
Population Size: 8
Sources: Page: table 2
Feeling abnormal 12.5%
500 mg single, oral
Recommended
Dose: 500 mg
Route: oral
Route: single
Dose: 500 mg
Sources: Page: table 2
healthy, 30-33 years
n = 8
Health Status: healthy
Age Group: 30-33 years
Sex: M+F
Population Size: 8
Sources: Page: table 2
Headache 12.5%
500 mg single, oral
Recommended
Dose: 500 mg
Route: oral
Route: single
Dose: 500 mg
Sources: Page: table 2
healthy, 30-33 years
n = 8
Health Status: healthy
Age Group: 30-33 years
Sex: M+F
Population Size: 8
Sources: Page: table 2
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
no
no
no (co-administration study)
Comment: flurbiprofen increased tecovirimat Cmax by 7% and AUC by 4%
Page: 24, 70, 72
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
Page: 24, 73
weak
no (co-administration study)
Comment: tecovirimat is an inducer of CYP2B6/2C9/3A4 activities at 100 uM
Page: 73.0
weak
yes (co-administration study)
Comment: tecovirimat increased omeprazole Cmax by 86% and AUC by 72%; tecovirimat is not a TDI of CYP2C19
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
Page: 2, 3, 10, 24, 70
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
Page: 2, 3, 10, 24, 73
yes [IC50 6.03 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no
no
no
no
no
no
yes
yes
yes (co-administration study)
Comment: tecovirimat exposures can be increased or decreased by the use of UGT1A1/4 inhibitor or inducers, respectively
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
Page: 10, 24, 68
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Patents

Sample Use Guides

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
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.
Name Type Language
TECOVIRIMAT MONOHYDRATE
MI  
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
TECOVIRIMAT MONOHYDRATE [WHO-DD]
Common Name English
ST-246 MONOHYDRATE
Code English
TECOVIRIMAT MONOHYDRATE [MI]
Common Name English
Code System Code Type Description
FDA UNII
SB96YO2BR8
Created by admin on Sat Jun 26 04:45:14 UTC 2021 , Edited by admin on Sat Jun 26 04:45:14 UTC 2021
PRIMARY
DRUG BANK
DBSALT002799
Created by admin on Sat Jun 26 04:45:14 UTC 2021 , Edited by admin on Sat Jun 26 04:45:14 UTC 2021
PRIMARY
PUBCHEM
90479083
Created by admin on Sat Jun 26 04:45:14 UTC 2021 , Edited by admin on Sat Jun 26 04:45:14 UTC 2021
PRIMARY
RXCUI
2055677
Created by admin on Sat Jun 26 04:45:14 UTC 2021 , Edited by admin on Sat Jun 26 04:45:14 UTC 2021
ALTERNATIVE
MERCK INDEX
M10514
Created by admin on Sat Jun 26 04:45:14 UTC 2021 , Edited by admin on Sat Jun 26 04:45:14 UTC 2021
PRIMARY Merck Index
CAS
1162664-19-8
Created by admin on Sat Jun 26 04:45:14 UTC 2021 , Edited by admin on Sat Jun 26 04:45:14 UTC 2021
PRIMARY
RXCUI
2055103
Created by admin on Sat Jun 26 04:45:14 UTC 2021 , Edited by admin on Sat Jun 26 04:45:14 UTC 2021
PRIMARY
EVMPD
SUB196827
Created by admin on Sat Jun 26 04:45:14 UTC 2021 , Edited by admin on Sat Jun 26 04:45:14 UTC 2021
PRIMARY