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Details

Stereochemistry ABSOLUTE
Molecular Formula C37H53NO8
Molecular Weight 639.82
Optical Activity UNSPECIFIED
Defined Stereocenters 10 / 10
E/Z Centers 2
Charge 0

SHOW SMILES / InChI
Structure of MOXIDECTIN

SMILES

CC(C)/C(/[H])=C(\C)/[C@]1([H])[C@@]([H])(C)/C(=N/OC)/C[C@]2(C[C@]3([H])C[C@@]([H])(C/C(/[H])=C(\C)/C[C@@]([H])(C)/C(/[H])=C(\[H])/C(/[H])=C/4\CO[C@]5([H])[C@@]([H])(C(=C[C@@]([H])(C(=O)O3)[C@]45O)C)O)O2)O1

InChI

InChIKey=YZBLFMPOMVTDJY-LSGXYNIPSA-N
InChI=1S/C37H53NO8/c1-21(2)14-25(6)33-26(7)31(38-42-8)19-36(46-33)18-29-17-28(45-36)13-12-23(4)15-22(3)10-9-11-27-20-43-34-32(39)24(5)16-30(35(40)44-29)37(27,34)41/h9-12,14,16,21-22,26,28-30,32-34,39,41H,13,15,17-20H2,1-8H3/b10-9+,23-12+,25-14+,27-11+,38-31+/t22-,26-,28+,29-,30-,32+,33+,34+,36-,37+/m0/s1

HIDE SMILES / InChI

Molecular Formula C37H53NO8
Molecular Weight 639.82
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 10 / 10
E/Z Centers 2
Optical Activity UNSPECIFIED

CNS Activity

Curator's Comment:: Safety assessments indicated that moxidectin was safe and well tolerated, with a slightly higher incidence of transient, mild, and moderate CNS adverse events (dizziness and somnolence) as compared to placebo.

Originator

Curator's Comment:: The first Moxidectin-containing product was an injectable formulation for cattle, approved for commercial use in Argentina in 1989. Additionally, an ongoing collaboration between Wyeth/Fort Dodge Animal Health and the World Health Organization led to the development of an oral formulation of MOX for humans, which is being evaluated in several African countries for prevention of river blindness, a parasitic disease caused by Onchocerca volvulus. # Wyeth Pharmaceuticals

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
Target ID: 176472.0
Gene Symbol: unc-49
0.18 nM [Kd]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Curative
MOXIDECTIN

Approved Use

Moxidectin is an anthelmintic indicated for the treatment of onchocerciasis due to Onchocerca volvulus in patients aged 12 years and older.

Launch Date

1.52876155E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
247 ng/mL
36 mg single, oral
dose: 36 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
56.7 ng/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
58.9 ng/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
79.1 ng/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: HIGH-FAT
63.1 ng/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
58.9 ng/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
133 ng/mL
16 mg single, oral
dose: 16 mg
route of administration: oral
experiment type: single
co-administered:
MOXIDECTIN plasma
Homo sapiens
176 ng/mL
24 mg single, oral
dose: 24 mg
route of administration: oral
experiment type: single
co-administered:
MOXIDECTIN plasma
Homo sapiens
247 ng/mL
36 mg single, oral
dose: 36 mg
route of administration: oral
experiment type: single
co-administered:
MOXIDECTIN plasma
Homo sapiens
27.2 ng/mL
4 mg single, oral
dose: 4 mg
route of administration: oral
experiment type: single
co-administered:
MOXIDECTIN plasma
Homo sapiens
56.7 ng/mL
8 mg single, oral
dose: 8 mg
route of administration: oral
experiment type: single
co-administered:
MOXIDECTIN plasma
Homo sapiens
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
2613 ng × h/mL
36 mg single, oral
dose: 36 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
632.6 ng × h/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: UNKNOWN
3387 ng × h/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
7885 ng × h/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: HIGH-FAT
2738 ng × h/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
3387 ng × h/mL
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
559 h
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
784 h
8 mg single, oral
dose: 8 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MOXIDECTIN plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: UNKNOWN
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Other AEs: Eosinophilia, Pruritus...
Other AEs:
Eosinophilia (74%)
Pruritus (65%)
Musculoskeletal pain (64%)
Headache (58%)
Lymphocytopenia (48%)
Tachycardia (39%)
Postural orthostatic tachycardia syndrome (34%)
Tachycardia (18%)
Rash (37%)
Abdominal pain (31%)
Sources: Page: 3
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Other AEs: Hypotension, Orthostatic hypotension...
Other AEs:
Hypotension (30%)
Orthostatic hypotension (22%)
Pyrexia (27%)
Leukocytosis (25%)
Influenza like illness (23%)
Neutropenia (20%)
Cough (17%)
Lymph node pain (13%)
Dizziness (12%)
Gastroenteritis (15%)
Hyponatremia (12%)
Peripheral swelling (11%)
Eye pain (8%)
Eye pruritus (7%)
Visual impairment (3%)
Eyelid edema (2%)
Conjunctivitis allergic (2%)
Ocular discomfort (2%)
Conjunctival hyperemia (2%)
Lacrimation increased (1%)
Sources: Page: 4
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 5
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 5
Other AEs: Eosinophilia, Lymphocytopenia...
Other AEs:
Eosinophilia (grade 4, 18%)
Lymphocytopenia (grade 3, 23%)
Neutrophils (grade 4, 7%)
Sources: Page: 5
18 mg single, oral
Recommended
Dose: 18 mg
Route: oral
Route: single
Dose: 18 mg
Sources: Page: 1111
healthy, 18-45 years
n = 5
Health Status: healthy
Age Group: 18-45 years
Sex: M
Population Size: 5
Sources: Page: 1111
Other AEs: Somnolence...
Other AEs:
Somnolence (20%)
Sources: Page: 1111
36 mg single, oral
Recommended
Dose: 36 mg
Route: oral
Route: single
Dose: 36 mg
Sources: Page: 1111
healthy, 18-45 years
n = 10
Health Status: healthy
Age Group: 18-45 years
Sex: M
Population Size: 10
Sources: Page: 1111
Other AEs: Somnolence...
Other AEs:
Somnolence (40%)
Sources: Page: 1111
2 mg single, oral
RP2D
Dose: 2 mg
Route: oral
Route: single
Dose: 2 mg
Sources: Page: 13
unhealthy, adult
n = 44
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 44
Sources: Page: 13
Other AEs: Generalized pruritus, Rash...
Other AEs:
Generalized pruritus (52%)
Rash (41%)
Postural orthostatic tachycardia syndrome (48%)
Orthostatic hypotension (18%)
Lymph node pain (20%)
Sources: Page: 13
4 mg single, oral
RP2D
Dose: 4 mg
Route: oral
Route: single
Dose: 4 mg
Sources: Page: 13
unhealthy, adult
n = 45
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 45
Sources: Page: 13
Other AEs: Generalized pruritus, Rash...
Other AEs:
Generalized pruritus (80%)
Rash (53%)
Postural orthostatic tachycardia syndrome (31%)
Orthostatic hypotension (29%)
Lymph node pain (36%)
Sources: Page: 13
8 mg single, oral
RP2D
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 13
unhealthy, adult
n = 38
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 38
Sources: Page: 13
Other AEs: Generalized pruritus, Rash...
Other AEs:
Generalized pruritus (88%)
Rash (63%)
Postural orthostatic tachycardia syndrome (63%)
Orthostatic hypotension (60%)
Lymph node pain (63%)
Sources: Page: 13
AEs

AEs

AESignificanceDosePopulation
Tachycardia 18%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Abdominal pain 31%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Postural orthostatic tachycardia syndrome 34%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Rash 37%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Tachycardia 39%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Lymphocytopenia 48%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Headache 58%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Musculoskeletal pain 64%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Pruritus 65%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Eosinophilia 74%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 3
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 3
Lacrimation increased 1%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Peripheral swelling 11%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Dizziness 12%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Hyponatremia 12%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Lymph node pain 13%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Gastroenteritis 15%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Cough 17%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Conjunctival hyperemia 2%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Conjunctivitis allergic 2%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Eyelid edema 2%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Ocular discomfort 2%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Neutropenia 20%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Orthostatic hypotension 22%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Influenza like illness 23%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Leukocytosis 25%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Pyrexia 27%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Visual impairment 3%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Hypotension 30%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Eye pruritus 7%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Eye pain 8%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 4
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 4
Lymphocytopenia grade 3, 23%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 5
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 5
Eosinophilia grade 4, 18%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 5
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 5
Neutrophils grade 4, 7%
8 mg single, oral
Recommended
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 5
unhealthy, 18 - 60 years
n = 978
Health Status: unhealthy
Condition: onchocerciasis
Age Group: 18 - 60 years
Sex: unknown
Population Size: 978
Sources: Page: 5
Somnolence 20%
18 mg single, oral
Recommended
Dose: 18 mg
Route: oral
Route: single
Dose: 18 mg
Sources: Page: 1111
healthy, 18-45 years
n = 5
Health Status: healthy
Age Group: 18-45 years
Sex: M
Population Size: 5
Sources: Page: 1111
Somnolence 40%
36 mg single, oral
Recommended
Dose: 36 mg
Route: oral
Route: single
Dose: 36 mg
Sources: Page: 1111
healthy, 18-45 years
n = 10
Health Status: healthy
Age Group: 18-45 years
Sex: M
Population Size: 10
Sources: Page: 1111
Orthostatic hypotension 18%
2 mg single, oral
RP2D
Dose: 2 mg
Route: oral
Route: single
Dose: 2 mg
Sources: Page: 13
unhealthy, adult
n = 44
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 44
Sources: Page: 13
Lymph node pain 20%
2 mg single, oral
RP2D
Dose: 2 mg
Route: oral
Route: single
Dose: 2 mg
Sources: Page: 13
unhealthy, adult
n = 44
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 44
Sources: Page: 13
Rash 41%
2 mg single, oral
RP2D
Dose: 2 mg
Route: oral
Route: single
Dose: 2 mg
Sources: Page: 13
unhealthy, adult
n = 44
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 44
Sources: Page: 13
Postural orthostatic tachycardia syndrome 48%
2 mg single, oral
RP2D
Dose: 2 mg
Route: oral
Route: single
Dose: 2 mg
Sources: Page: 13
unhealthy, adult
n = 44
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 44
Sources: Page: 13
Generalized pruritus 52%
2 mg single, oral
RP2D
Dose: 2 mg
Route: oral
Route: single
Dose: 2 mg
Sources: Page: 13
unhealthy, adult
n = 44
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 44
Sources: Page: 13
Orthostatic hypotension 29%
4 mg single, oral
RP2D
Dose: 4 mg
Route: oral
Route: single
Dose: 4 mg
Sources: Page: 13
unhealthy, adult
n = 45
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 45
Sources: Page: 13
Postural orthostatic tachycardia syndrome 31%
4 mg single, oral
RP2D
Dose: 4 mg
Route: oral
Route: single
Dose: 4 mg
Sources: Page: 13
unhealthy, adult
n = 45
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 45
Sources: Page: 13
Lymph node pain 36%
4 mg single, oral
RP2D
Dose: 4 mg
Route: oral
Route: single
Dose: 4 mg
Sources: Page: 13
unhealthy, adult
n = 45
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 45
Sources: Page: 13
Rash 53%
4 mg single, oral
RP2D
Dose: 4 mg
Route: oral
Route: single
Dose: 4 mg
Sources: Page: 13
unhealthy, adult
n = 45
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 45
Sources: Page: 13
Generalized pruritus 80%
4 mg single, oral
RP2D
Dose: 4 mg
Route: oral
Route: single
Dose: 4 mg
Sources: Page: 13
unhealthy, adult
n = 45
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 45
Sources: Page: 13
Orthostatic hypotension 60%
8 mg single, oral
RP2D
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 13
unhealthy, adult
n = 38
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 38
Sources: Page: 13
Lymph node pain 63%
8 mg single, oral
RP2D
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 13
unhealthy, adult
n = 38
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 38
Sources: Page: 13
Postural orthostatic tachycardia syndrome 63%
8 mg single, oral
RP2D
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 13
unhealthy, adult
n = 38
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 38
Sources: Page: 13
Rash 63%
8 mg single, oral
RP2D
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 13
unhealthy, adult
n = 38
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 38
Sources: Page: 13
Generalized pruritus 88%
8 mg single, oral
RP2D
Dose: 8 mg
Route: oral
Route: single
Dose: 8 mg
Sources: Page: 13
unhealthy, adult
n = 38
Health Status: unhealthy
Condition: onchocerciasis
Age Group: adult
Sex: unknown
Population Size: 38
Sources: Page: 13
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no
no
no
no
no
no (co-administration study)
Comment: no in vivo drug-drug interaction between moxidectin and the CYP3A4 substrate, midazolam
Page: 8;12;43;53
weak [IC50 10 uM]
weak [IC50 145 uM]
weak [IC50 459 uM]
weak
weak
yes
no (co-administration study)
Comment: no in vivo drug-drug interaction between moxidectin and the CYP3A4 substrate, midazolam; with
Page: 8;12;43;53
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
limited
limited
limited
major
major
no
no
weak
yes
yes
yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Cloning of an avermectin-sensitive glutamate-gated chloride channel from Caenorhabditis elegans.
1994 Oct 20
A glutamate-gated chloride channel subunit from Haemonchus contortus: expression in a mammalian cell line, ligand binding, and modulation of anthelmintic binding by glutamate.
2002 Mar 15
The antiparasitic moxidectin: safety, tolerability, and pharmacokinetics in humans.
2003 Oct
Glutamate-gated chloride channels and the mode of action of the avermectin/milbemycin anthelmintics.
2005
Moxidectin: a review of chemistry, pharmacokinetics and use in horses.
2009 Sep 25
Relative neurotoxicity of ivermectin and moxidectin in Mdr1ab (-/-) mice and effects on mammalian GABA(A) channel activity.
2012
Pharmacological characterization of the Haemonchus contortus GABA-gated chloride channel, Hco-UNC-49: modulation by macrocyclic lactone anthelmintics and a receptor for piperazine.
2012 Apr 30
Moxidectin and the avermectins: Consanguinity but not identity.
2012 Dec
Moxidectin has a lower neurotoxic potential but comparable brain penetration in P-glycoprotein-deficient CF-1 mice compared to ivermectin.
2013 Jun
The potential impact of moxidectin on onchocerciasis elimination in Africa: an economic evaluation based on the Phase II clinical trial data.
2015 Mar 19
Patents

Sample Use Guides

In Vivo Use Guide
Curator's Comment:: Moxidectin is safe and well tolerated in humans after single, oral doses of 3 mg to 36 mg.
single doses of 50 µg/kg to 600 µg/kg
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment:: Modulation of Hco-UNC-49 (Haemonchus contortus GABA-gated chloride channel) by moxidectin was tested to determine the effect of these molecules on the Hco-UNC-49 channel. Moxidectin alone does not produce currents at the concentration 10 uM. However, during co-application of moxidectin (10 uM) with 50 uM of GABA, both the homomeric (Hco-UNC-49B; p<0.05) and heteromeric (Hco-UNC-49B/C; p<0.01) Hco-UNC-49 channels displayed an enhanced response.
Xenopus laevis oocytes, 10 µM
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:19:25 UTC 2021
Edited
by admin
on Fri Jun 25 21:19:25 UTC 2021
Record UNII
NGU5H31YO9
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
MOXIDECTIN
GREEN BOOK   INN   MART.   MI   USAN   USP-RS  
INN   USAN  
Official Name English
MOXIDECTIN [ORANGE BOOK]
Common Name English
NSC-760424
Code English
MOXIDECTIN [MI]
Common Name English
ADVOCATE COMPONENT MOXIDECTIN
Brand Name English
MOXIDECTIN [MART.]
Common Name English
MOXIDECTIN [EMA EPAR: VETERINARY]
Common Name English
MOXIDECTIN [INN]
Common Name English
MOXIDECTIN FOR VETERINARY USE [EP MONOGRAPH]
Common Name English
MOXIDECTIN [USAN]
Common Name English
MOXIDECTIN [USP MONOGRAPH]
Common Name English
MOXIDECTIN COMPONENT OF ADVOCATE
Brand Name English
MOXIDECTIN [USP-RS]
Common Name English
CL 301,423
Code English
MILBEMYCIN B, 5-O-DEMETHYL-28-DEOXY-25-(1,3-DIMETHYL-1-BUTENYL)-6,28-EPOXY-23-(METHOXYIMINO)-,(6R,23E,25S(E))-
Common Name English
(6R,25S)-5-O-DEMETHYL-28-DEOXY-25-((E)-1,3-DIMETHYL-1-BUTENYL)-6,28-EPOXY-23-OXOMILBEMYCIN B23-(E)-(O-METHYLOXIME)
Common Name English
CL-301,423
Code English
MOXIDECTIN [WHO-DD]
Common Name English
MOXIDECTIN [GREEN BOOK]
Common Name English
Classification Tree Code System Code
EMA VETERINARY ASSESSMENT REPORTS ADVOCATE [AUTHORISED]
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
FDA ORPHAN DRUG 316510
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
WHO-VATC QP54AB02
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
WHO-VATC QP54AB52
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
CFR 21 CFR 556.426
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
CFR 21 CFR 520.1452
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
CFR 21 CFR 524.1450
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
CFR 21 CFR 522.1450
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
CFR 21 CFR 522.1451
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
CFR 21 CFR 524.1146
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
CFR 21 CFR 520.1454
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
CFR 21 CFR 520.1453
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
EMA VETERINARY ASSESSMENT REPORTS ADVOCATE [AUTHORISED]
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
CFR 21 CFR 520.1451
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
EMA VETERINARY ASSESSMENT REPORTS ADVOCATE [AUTHORISED]
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
Code System Code Type Description
DRUG BANK
DB11431
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
RXCUI
1047072
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY RxNorm
INN
6400
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
NCI_THESAURUS
C73264
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
CAS
113507-06-5
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
DRUG CENTRAL
5286
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
WIKIPEDIA
MOXIDECTIN
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
MESH
C027837
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
PUBCHEM
9832912
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
MERCK INDEX
M7646
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY Merck Index
EPA CompTox
113507-06-5
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
USP_CATALOG
1448559
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY USP-RS
ChEMBL
CHEMBL2104415
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
EVMPD
SUB09085MIG
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
FDA UNII
NGU5H31YO9
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
LACTMED
Moxidectin
Created by admin on Fri Jun 25 21:19:25 UTC 2021 , Edited by admin on Fri Jun 25 21:19:25 UTC 2021
PRIMARY
Related Record Type Details
TRANSPORTER -> INHIBITOR
BASIS OF STRENGTH->SUBSTANCE
ASSAY (HPLC)
EP
METABOLIC ENZYME -> INDUCER
CYP3A4 expression was also induced by rifampin by a mean value of approximately 43-fold compared to vehicle control values
INDUCER
MAY BE CLINICALLY SIGNIFICANT
TARGET ORGANISM->INHIBITOR
EXCRETED UNCHANGED
No human mass balance study was conducted due to long half-life. Feces: 2% dose within the first 72 hours after 8 mg dose;
Related Record Type Details
METABOLITE -> PARENT
METABOLITE -> PARENT
METABOLITE -> PARENT
Related Record Type Details
IMPURITY -> PARENT
TEST A; sum of impurities E and F: not more than 1.7 times the area of the principal peak in the chromatogram obtained with reference solution (a) (1.7 per cent)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
TEST B
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
TEST A
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
TEST A
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
UNSPECIFIED
EP
IMPURITY -> PARENT
TEST A
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
TEST A
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
TEST B; sum of impurities H and I: not more than the area of the principal peak in the chromatogram obtained with reference solution (a) (1.0 per cent)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
TEST B
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
TEST A; sum of impurities E and F: not more than 1.7 times the area of the principal peak in the chromatogram obtained with reference solution (a) (1.7 per cent)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
TEST B; sum of impurities H and I: not more than the area of the principal peak in the chromatogram obtained with reference solution (a) (1.0 per cent)
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
IMPURITY -> PARENT
TEST A
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Cmax PHARMACOKINETIC DOSAGE
PHARMACOKINETIC
ROUTE OF ADMINISTRATION
PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Tmax DOSAGE
PHARMACOKINETIC
ROUTE OF ADMINISTRATION
PHARMACOKINETIC