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Details

Stereochemistry ABSOLUTE
Molecular Formula C32H30F5N3O5
Molecular Weight 631.5909
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ELAGOLIX

SMILES

Cc1c(-c2cccc(c2F)OC)c(=O)n(C[C@@]([H])(c3ccccc3)NCCCC(=O)O)c(=O)n1Cc4c(cccc4F)C(F)(F)F

InChI

InChIKey=HEAUOKZIVMZVQL-VWLOTQADSA-N
InChI=1S/C32H30F5N3O5/c1-19-28(21-11-6-14-26(45-2)29(21)34)30(43)40(18-25(20-9-4-3-5-10-20)38-16-8-15-27(41)42)31(44)39(19)17-22-23(32(35,36)37)12-7-13-24(22)33/h3-7,9-14,25,38H,8,15-18H2,1-2H3,(H,41,42)/t25-/m0/s1

HIDE SMILES / InChI

Molecular Formula C32H30F5N3O5
Molecular Weight 631.5909
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 1 / 1
E/Z Centers 0
Optical Activity UNSPECIFIED

Elagolix (ABT-620) is an oral gonadotropin-releasing hormone antagonist being studied for the treatment of endometriosis and uterine fibroids. The U.S. Food and Drug Administration (FDA) approved AbbVie's elagolix under the brand name Orilissa as the first and only oral gonadotropin-releasing hormone (GnRH) antagonist specifically developed for women with moderate to severe endometriosis pain.

CNS Activity

Curator's Comment:: Elagolix did not cross the blood brain barrier.

Approval Year

TargetsConditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Orilissa

Approved Use

ORILISSA is a gonadotropin -releasing hormone (GnRH) receptor antagonist indicated for the management of moderate to severe pain associated with endometriosis .

Launch Date

1532304000000
Primary
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
1314 ng/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELAGOLIX plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
3231 ng × h/mL
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELAGOLIX plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.48 h
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ELAGOLIX plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
Doses

Doses

DosePopulationAdverse events​
400 mg single, oral
Highest studied dose
Dose: 400 mg
Route: oral
Route: single
Dose: 400 mg
Sources:
healthy, 18 –39 years
Health Status: healthy
Age Group: 18 –39 years
Sources:
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (0.8%)
Vomiting (0.6%)
Headache (0.8%)
Depression (0.4%)
Hot flush (0.8%)
Insomnia (0.4%)
Irritability (0.4%)
Mood swings (0.4%)
Abdominal pain (0.2%)
Acne (0.2%)
Endometriosis (0.4%)
Migraine (0.2%)
Sources:
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Disc. AE: Nausea, Vomiting...
AEs leading to
discontinuation/dose reduction:
Nausea (1.5%)
Vomiting (0.4%)
Headache (1%)
Depression (0.6%)
Hot flush (2.5%)
Insomnia (0.4%)
Irritability (0.4%)
Mood swings (0.2%)
Abdominal pain (0.4%)
Acne (0.4%)
Facial swelling (0.4%)
Migraine (0.4%)
Depressed mood (0.4%)
Diarrhea (0.6%)
ALT increased (0.4%)
AST increased (0.4%)
Arthralgia (0.6%)
Rash (0.4%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Abdominal pain 0.2%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Acne 0.2%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Migraine 0.2%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Depression 0.4%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Endometriosis 0.4%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Insomnia 0.4%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Irritability 0.4%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Mood swings 0.4%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Vomiting 0.6%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Headache 0.8%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Hot flush 0.8%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Nausea 0.8%
Disc. AE
150 mg 1 times / day steady, oral
Recommended
Dose: 150 mg, 1 times / day
Route: oral
Route: steady
Dose: 150 mg, 1 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Mood swings 0.2%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
ALT increased 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
AST increased 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Abdominal pain 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Acne 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Depressed mood 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Facial swelling 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Insomnia 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Irritability 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Migraine 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Rash 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Vomiting 0.4%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Arthralgia 0.6%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Depression 0.6%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Diarrhea 0.6%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Headache 1%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Nausea 1.5%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
Hot flush 2.5%
Disc. AE
200 mg 2 times / day steady, oral
Recommended
Dose: 200 mg, 2 times / day
Route: oral
Route: steady
Dose: 200 mg, 2 times / day
Sources:
unhealthy, adult (premenopausal women)
Health Status: unhealthy
Age Group: adult (premenopausal women)
Sex: F
Sources:
OverviewDrug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
no [IC50 145 uM]
no [IC50 150 uM]
no [IC50 161 uM]
no [IC50 280 uM]
no [IC50 45 uM]
no [IC50 >100 uM]
no [IC50 >300 uM]
weak [IC50 >29 uM]
weak [IC50 >29 uM]
weak [IC50 >30 uM]
weak [IC50 >30 uM]
weak [IC50 >30 uM]
weak [IC50 >30 uM]
yes [IC50 1.7 uM]
yes (co-administration study)
Comment: BCRP/OATP1B1 inhibition by elagolix 300 mg BID ↓AUC by 40% ↔ Cmax (rosuvastatin)
Page: 41
yes [IC50 19 uM]
yes [IC50 36 uM]
yes [IC50 4.7 uM]
yes [IC50 54 uM]
yes [Ki 34 uM]
yes [Ki 74 uM]
yes
yes
yes
yes
yes
yes
yes (co-administration study)
Comment: CYP3A4 induction by elagolix 150 mg QD and 300 mg BID ↓AUC by 35 - 55% ↓Cmax by 19 – 44% (midazolam)
Page: 41
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
no
no
no
yes
yes
yes
yes
likely (co-administration study)
Comment: CYP3A4/P-gp induction by rifampin, 600 mg QD ↑Cmax by 100% ↑AUC by 65%
Page: 41
yes
yes (co-administration study)
Comment: CYP3A4 inhibition by ketoconazole, 400 mg QD ↑Cmax by 77% ↑AUC by 120%
Page: 41
yes
yes (co-administration study)
Comment: OATP1B1 inhibition by a single dose of rifampin, 600 mg ↑Cmax by 337% ↑AUC by 458%
Page: 41
Tox targets
PubMed

PubMed

TitleDatePubMed
Discovery of sodium R-(+)-4-{2-[5-(2-fluoro-3-methoxyphenyl)-3-(2-fluoro-6-[trifluoromethyl]benzyl)-4-methyl-2,6-dioxo-3,6-dihydro-2H-pyrimidin-1-yl]-1-phenylethylamino}butyrate (elagolix), a potent and orally available nonpeptide antagonist of the human gonadotropin-releasing hormone receptor.
2008 Dec 11
Discovery of 1-{4-[1-(2,6-difluorobenzyl)-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-6-yl]phenyl}-3-methoxyurea (TAK-385) as a potent, orally active, non-peptide antagonist of the human gonadotropin-releasing hormone receptor.
2011 Jul 28
Patents

Sample Use Guides

Normal liver function or mild hepatic impairment : 150 mg once daily
Route of Administration: Oral
Elagolix displays high affinity in a competition binding assay for hGnRH-R (Ki = 0.90 nM) and low CYP3A4 inhibition (IC50 = 56 uM). It is a slowly disassociating antagonist exhibiting very high affinity (KD = 54 pM) and insurmountable antagonism. Elagolix is highly selective at hGnRH-R, its wider receptor selectivity is tested at a concentration of 10 uM in a panel of radioligand binding assays for 100 off-target receptors, ion channels, enzymes, and transporters, and significant activity is not observed (inhibition <50%). It does not stimulate histamine release from cultured rat peritoneal mast cells.
Substance Class Chemical
Created
by admin
on Sat Jun 26 12:06:20 UTC 2021
Edited
by admin
on Sat Jun 26 12:06:20 UTC 2021
Record UNII
5B2546MB5Z
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ELAGOLIX
INN   MI   USAN   WHO-DD  
USAN   INN  
Official Name English
ELAGOLIX [INN]
Common Name English
ELAGOLIX [USAN]
Common Name English
ELAGOLIX [WHO-DD]
Common Name English
NBI-56418
Code English
4-(((1R)-2-(5-(2-FLUORO-3-METHOXYPHENYL)-3-((2-FLUORO-6-(TRIFLUOROMETHYL)PHENYL)METHYL)- 4-METHYL-2,6-DIOXO-3,6-DIHYDROPYRIMIDIN-1(2H)-YL)-1-PHENYLETHYL)AMINO)BUTANOIC ACID
Systematic Name English
ELAGOLIX [MI]
Common Name English
BUTANOIC ACID, 4-(((1R)-2-(5-(2-FLUORO-3-METHOXYPHENYL)-3-((2-FLUORO-6-(TRIFLUOROMETHYL)PHENYL)METHYL)-3,6-DIHYDRO-4-METHYL-2,6-DIOXO-1(2H)-PYRIMIDINYL)-1- PHENYLETHYL)AMINO)-
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C241
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
NCI_THESAURUS C2092
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
Code System Code Type Description
DRUG CENTRAL
5293
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
CAS
834153-87-6
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
EPA CompTox
834153-87-6
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
LACTMED
Elagolix
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
MERCK INDEX
M4850
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY Merck Index
WIKIPEDIA
Elagolix
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
FDA UNII
5B2546MB5Z
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
NCI_THESAURUS
C153373
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
PUBCHEM
11250647
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
MESH
C539351
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
DRUG BANK
DB11979
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
INN
8983
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
RXCUI
2049846
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
ChEMBL
CHEMBL1208155
Created by admin on Sat Jun 26 12:06:21 UTC 2021 , Edited by admin on Sat Jun 26 12:06:21 UTC 2021
PRIMARY
Related Record Type Details
TARGET -> INHIBITOR
Ki
TRANSPORTER -> INHIBITOR
TARGET -> INDUCER
SALT/SOLVATE -> PARENT
TARGET -> INDUCER
TARGET -> INHIBITOR
Ki
TARGET -> INDUCER
TRANSPORTER -> INHIBITOR
TRANSPORTER -> INHIBITOR
EXCRETED UNCHANGED
URINE
TARGET -> INDUCER
TRANSPORTER -> SUBSTRATE
EXCRETED UNCHANGED
FECAL
TARGET -> INDUCER
TRANSPORTER -> INHIBITOR
TARGET -> INHIBITOR
Ki
METABOLIC ENZYME -> SUBSTRATE
MAJOR
TRANSPORTER -> SUBSTRATE
BINDER->LIGAND
METABOLIC ENZYME -> SUBSTRATE
MINOR
TARGET -> INHIBITOR
Ki
METABOLIC ENZYME -> SUBSTRATE
MAJOR
Related Record Type Details
METABOLITE -> PARENT
Related Record Type Details
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Volume of Distribution PHARMACOKINETIC DOSE

Biological Half-life PHARMACOKINETIC DOSE

Tmax PHARMACOKINETIC DOSE