BILASTINE

Possibly Marketed Outside US

Details

Stereochemistry	ACHIRAL
Molecular Formula	C28H37N3O3
Molecular Weight	463.6117
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CCOCCN1C(=NC2=C1C=CC=C2)C3CCN(CCC4=CC=C(C=C4)C(C)(C)C(O)=O)CC3

InChI

InChIKey=ACCMWZWAEFYUGZ-UHFFFAOYSA-N

InChI=1S/C28H37N3O3/c1-4-34-20-19-31-25-8-6-5-7-24(25)29-26(31)22-14-17-30(18-15-22)16-13-21-9-11-23(12-10-21)28(2,3)27(32)33/h5-12,22H,4,13-20H2,1-3H3,(H,32,33)

HIDE SMILES / InChI

Molecular Formula	C28H37N3O3
Molecular Weight	463.6117
Charge	0
Count

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

Description
Sources: https://www.medicines.org.uk/emc/PIL.24462.latest.pdf
Curator's Comment: description was created based on several sources, including: https://www.ncbi.nlm.nih.gov/pubmed/25878559 | https://medical.azureedge.net/pdf/28433.pdf?v=636220857643656872 | https://www.faesfarma.com/wp-content/uploads/2015/07/AI-20110329-EN.pdf

Bilastine is a new second generation H1-antihistamine recently approved for the symptomatic treatment of allergic rhinitis (AR) and chronic urticaria (CU). Bilastine is an H1 receptor inverse agonist. Bilastine also exerts anti-inflammatory activity by inhibiting the release of histamine, IL-4 and tumor necrosis factor (TNF)-α from human mast cells and granulocytes. Common side effects are headache and drowsiness.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histamine H1 receptor 316 Target ID: CHEMBL231 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16274260 \| https://www.ncbi.nlm.nih.gov/pubmed/25878559	Inverse Agonist 85		64.0 nM [Ki]

Conditions

Condition	Modality	Highest Phase	Product
Allergic rhinitis 104 Sources: https://www.medicines.org.uk/emc/PIL.24462.latest.pdf	Palliative	Approved 8583	Bilaxten Approved Use Bilastine is used to relieve the symptoms of hayfever (sneezing, itchy, runny, blocked-up nose and red and watery eyes) and other forms of allergic rhinitis. It may also be used to treat itchy skin rashes (hives or urticaria). Launch Date 2010
Hayfever 1 Sources: https://www.medicines.org.uk/emc/PIL.24462.latest.pdf	Palliative	Approved 8583	Bilaxten Approved Use Bilastine is used to relieve the symptoms of hayfever (sneezing, itchy, runny, blocked-up nose and red and watery eyes) and other forms of allergic rhinitis. It may also be used to treat itchy skin rashes (hives or urticaria). Launch Date 2010
Urticaria 39 Sources: https://www.medicines.org.uk/emc/PIL.24462.latest.pdf	Palliative	Approved 8583	Bilaxten Approved Use Bilastine is used to relieve the symptoms of hayfever (sneezing, itchy, runny, blocked-up nose and red and watery eyes) and other forms of allergic rhinitis. It may also be used to treat itchy skin rashes (hives or urticaria). Launch Date 2010

C_max

Value	Dose	Analyte	Population
277.9 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_K101_1.pdf.pdf#page=48	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
120.2 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_K101_1.pdf.pdf#page=48	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
153 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=86	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
275 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=86	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
756 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=86	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
345 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=24 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=93	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
341 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=24 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=93	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
949 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=24 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=93	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1006 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=24 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=93	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
59.6 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
135 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
761 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1419 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
106 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
99.1 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
232 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
182 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
821 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
740 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1580 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1278 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
273 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=125	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
410 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=125	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
195 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=126	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
226 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=126	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
144 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
172.1 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
271.1 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
228.8 ng/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
1284 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_K101_1.pdf.pdf#page=48	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
770.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_K101_1.pdf.pdf#page=48	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
681 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=86	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1373 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=86	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3435 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=86	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1439 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=24 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=93	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1551 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=24 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=93	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
3992 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=24 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=93	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
4474 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=24 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=93	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
326 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
693 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3348 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5153 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
506 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
454 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
990 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
876 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2982 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3087 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5675 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5109 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1205 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=125	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1483 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=125	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
1213 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=126	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1195 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=126	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
732.8 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
946.9 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1378.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1654.6 ng × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
10.54 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_K101_1.pdf.pdf#page=48	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.58 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_K101_1.pdf.pdf#page=48	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: HIGH-FAT
13.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=86	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=86	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=23 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=86	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
30.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
14.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
14.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
17.9 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=118	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.33 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.76 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	10 mg 1 times / day multiple, oral dose: 10 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.57 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.63 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.57 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
9.66 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	50 mg 1 times / day multiple, oral dose: 50 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.03 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.2 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=25 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=121	100 mg 1 times / day multiple, oral dose: 100 mg route of administration: Oral experiment type: MULTIPLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
13.11 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=125	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
10.35 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=125	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
11.8 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=126	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
11.22 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=126	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE food status: FASTED
9.26 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
15.1 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
10.5 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
18.4 h OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=26 \| https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=130	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	BILASTINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
10% OTHER GOV'T https://www.pmda.go.jp/drugs/2016/P20161025003/400107000_22800AMX00690000_A100_2.pdf#page=13			BILASTINE plasma	Homo sapiens

Doses

Dose	Population	Adverse events
200 mg 1 times / day multiple, oral Highest studied dose Dose: 200 mg, 1 times / day Route: oral Route: multiple Dose: 200 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/19705924/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19705924/	Sources: https://pubmed.ncbi.nlm.nih.gov/19705924/
220 mg single, oral Highest studied dose Dose: 220 mg Route: oral Route: single Dose: 220 mg Sources: https://pubmed.ncbi.nlm.nih.gov/19705924/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/19705924/	Sources: https://pubmed.ncbi.nlm.nih.gov/19705924/

PubMed

Title	Date	PubMed
Corrigendum to "Application of Analytical Quality by Design concept for bilastine and its degradation impurities determination by hydrophilic interaction liquid chromatographic method" [J. Pharm. Biomed. Anal. 125 (2016) 385-393].	2017-05-10	28249713
Bilastine in allergic rhinoconjunctivitis and urticaria: a practical approach to treatment decisions based on queries received by the medical information department.	2017	28210286
Comparative efficacy of bilastine, levocetirizine and desloratadine updosing in chronic urticaria.	2016	27932886

Patents

Sample Use Guides

In Vivo Use Guide

20 mg daily

Route of Administration: Oral

In Vitro Use Guide

Bilastine gave mild positive results for two uptake transporters, OATP2B1 and OCT1, mainly located in liver and intestine. Bilastine IC50 was determined for these two transporters and (based in previous knowledge), also for P-gp. The assay was carried out at seven bilastine concentrations ranging from 0.41 to 300 M. Bilastine showed poor inhibition, as values of IC50 obtained for all the three transporters were ≥ 300 M.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:02:04 GMT 2025` Edited by `admin` on `Mon Mar 31 18:02:04 GMT 2025`
Record UNII	PA1123N395
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

BILASTINE

Official Name

English

BILASTINE [MI]

Preferred Name

English

Bilastine [WHO-DD]

Common Name

English

BILASTINE [JAN]

Common Name

English

P-(2-(4-(1-(2-ETHOXYETHYL)-2-BENZIMIDAZOLYL)PIPERIDINO)ETHYL)-.ALPHA.-METHYLHYDRATROPIC ACID

Common Name

English

bilastine [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29578