BERAPROST

Possibly Marketed Outside US

Details

Stereochemistry	EPIMERIC
Molecular Formula	C24H30O5
Molecular Weight	398.492
Optical Activity	UNSPECIFIED
Defined Stereocenters	5 / 6
E/Z Centers	1
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC#CCC(C)[C@H](O)\C=C\[C@H]1[C@H](O)C[C@@H]2OC3=C(CCCC(O)=O)C=CC=C3[C@H]12

InChI

InChIKey=CTPOHARTNNSRSR-APJZLKAGSA-N

InChI=1S/C24H30O5/c1-3-4-7-15(2)19(25)13-12-17-20(26)14-21-23(17)18-10-5-8-16(24(18)29-21)9-6-11-22(27)28/h5,8,10,12-13,15,17,19-21,23,25-26H,6-7,9,11,14H2,1-2H3,(H,27,28)/b13-12+/t15?,17-,19+,20+,21-,23-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C24H30O5
Molecular Weight	398.492
Charge	0
Count

Stereochemistry	EPIMERIC
Additional Stereochemistry	No
Defined Stereocenters	5 / 6
E/Z Centers	1
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11790158
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/26686607 | https://www.ncbi.nlm.nih.gov/pubmed/2665758 | http://www.astellas.co.id/product/view/4/5

Beraprost is a stable, orally active prostacyclin analogue. Beraprost acts by binding to prostacyclin membrane receptors ultimately inhibiting the release of Ca2+ from intracellular storage sites. This reduction in the influx of Ca2+ has been postulated to cause relaxation of the smooth muscle cells and vasodilation. Beraprost is indicated for the treatment of pulmonary hypertension and improvement of ulcers, pain & feeling of coldness associated with chronic arterial occlusion. In addition beraprost displays thyroid hormone receptor antagonistic properties.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Prostanoid IP receptor 19 Target ID: CHEMBL1995 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2665758 \| https://www.ncbi.nlm.nih.gov/pubmed/10508233	Agonist 2752	133.0 nM [Kd]
Prostacyclin receptor 9 Target ID: P43252 Gene ID: 19222.0 Gene Symbol: Ptgir Target Organism: Mus musculus (Mouse) Sources: https://www.ncbi.nlm.nih.gov/pubmed/10508233	Agonist 2752	16.0 nM [Ki]
Prostanoid EP3 receptor 11 Target ID: CHEMBL4336 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10508233	Agonist 2752	110.0 nM [Ki]
Thyroid hormone receptor 6 Target ID: CHEMBL2111462 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26686607	Antagonist 2849	63.0 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Primary pulmonary hypertension 4 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11790158	Primary		Approved 8583	DORNER Approved Use Improvement of ulcers, pain & feeling of coldness associated with chronic arterial occlusion. Primary pulmonary Hypertension.
Chronic arterial occlusion 5 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11790158	Primary		Approved 8583	DORNER Approved Use Improvement of ulcers, pain & feeling of coldness associated with chronic arterial occlusion. Primary pulmonary Hypertension.

C_max

Value	Dose	Analyte	Population
84.9 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
119.8 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
190.6 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
240.2 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
22.4 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
30.8 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
46.68 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
54.4 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
97.1 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=11	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
27.7 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=11	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
485.6 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=11	40 μg single, oral dose: 40 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
184.3 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=11	40 μg single, oral dose: 40 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
170.4 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	120 μg 2 times / day multiple, oral dose: 120 μg route of administration: Oral experiment type: MULTIPLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
214.7 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	120 μg 2 times / day steady-state, oral dose: 120 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
46.7 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	120 μg 2 times / day multiple, oral dose: 120 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
45.3 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	120 μg 2 times / day steady-state, oral dose: 120 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
228.4 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	40 μg 3 times / day multiple, oral dose: 40 μg route of administration: Oral experiment type: MULTIPLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
242.2 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	40 μg 3 times / day steady-state, oral dose: 40 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
67.6 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	40 μg 3 times / day multiple, oral dose: 40 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
66.7 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	40 μg 3 times / day steady-state, oral dose: 40 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
178.5 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
113.2 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
56 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
35.1 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
264.5 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	180 μg single, oral dose: 180 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
177.4 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	180 μg single, oral dose: 180 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
77 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	180 μg single, oral dose: 180 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
42.3 pg/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	180 μg single, oral dose: 180 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.44 ng/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/480220_3399005F1021_1_A07_1F.pdf#page=21	50 μg single, oral dose: 50 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
57.7 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	20 μg single, oral dose: 20 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
122.4 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	40 μg single, oral dose: 40 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
185 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	60 μg single, oral dose: 60 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
40.4 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	20 μg 3 times / day multiple, oral dose: 20 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
122 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	40 μg 3 times / day multiple, oral dose: 40 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
150.6 pg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	60 μg 3 times / day multiple, oral dose: 60 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
978 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1252 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1862 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1766 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
155 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
226 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
341 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
328.98 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1119 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=11	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
234 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=11	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
717 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=11	40 μg single, oral dose: 40 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
159 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=11	40 μg single, oral dose: 40 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
810 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	120 μg 2 times / day multiple, oral dose: 120 μg route of administration: Oral experiment type: MULTIPLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1225 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	120 μg 2 times / day steady-state, oral dose: 120 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
190 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	120 μg 2 times / day multiple, oral dose: 120 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
221 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	120 μg 2 times / day steady-state, oral dose: 120 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
462 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	40 μg 3 times / day multiple, oral dose: 40 μg route of administration: Oral experiment type: MULTIPLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
550 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	40 μg 3 times / day steady-state, oral dose: 40 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
105 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	40 μg 3 times / day multiple, oral dose: 40 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
115 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K100_1.pdf#page=12	40 μg 3 times / day steady-state, oral dose: 40 μg route of administration: Oral experiment type: STEADY-STATE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1076 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
1073 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
233 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
214 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1989 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	180 μg single, oral dose: 180 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
2242 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	180 μg single, oral dose: 180 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
360 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	180 μg single, oral dose: 180 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
355 pg × h/mL OTHER GOV'T https://www.pmda.go.jp/drugs/2007/P200700047/48022000_21900AMX01753_K101_1.pdf#page=4	180 μg single, oral dose: 180 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.66 ng × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/480220_3399005F1021_1_A07_1F.pdf#page=21	50 μg single, oral dose: 50 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
44.5 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	20 μg single, oral dose: 20 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
105.6 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	40 μg single, oral dose: 40 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
168.7 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	60 μg single, oral dose: 60 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
43.4 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	20 μg 3 times / day multiple, oral dose: 20 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
108.6 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	40 μg 3 times / day multiple, oral dose: 40 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
184.9 pg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	60 μg 3 times / day multiple, oral dose: 60 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
14.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
13.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
18.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
19.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
15.48 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
8.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/	120 μg single, oral dose: 120 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
1.11 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/1/480220_3399005F1021_1_A07_1F.pdf#page=21	50 μg single, oral dose: 50 μg route of administration: Oral experiment type: SINGLE co-administered:	BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
0.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	20 μg single, oral dose: 20 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.53 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	40 μg single, oral dose: 40 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.62 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	60 μg single, oral dose: 60 μg route of administration: Oral experiment type: SINGLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.62 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	20 μg 3 times / day multiple, oral dose: 20 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.64 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	40 μg 3 times / day multiple, oral dose: 40 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN
0.91 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/7506323/	60 μg 3 times / day multiple, oral dose: 60 μg route of administration: Oral experiment type: MULTIPLE co-administered:	ESUBERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
8.4% EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/27681484/			BERAPROST plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
120 ug 2 times / day multiple, oral Higher than recommended Dose: 120 ug, 2 times / day Route: oral Route: multiple Dose: 120 ug, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31119846/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/31119846/	Other AEs: Headache, Diarrhea... Other AEs: Headache (8.7%) Diarrhea (2.7%) Hypertension (2%) Sources: https://pubmed.ncbi.nlm.nih.gov/31119846/
200 ug 4 times / day multiple, oral Higher than recommended Dose: 200 ug, 4 times / day Route: oral Route: multiple Dose: 200 ug, 4 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12821234/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: https://pubmed.ncbi.nlm.nih.gov/12821234/	Disc. AE: Nausea... AEs leading to discontinuation/dose reduction: Nausea (3%) Sources: https://pubmed.ncbi.nlm.nih.gov/12821234/

AEs

AE	Significance	Dose	Population
Hypertension	2%	120 ug 2 times / day multiple, oral Higher than recommended Dose: 120 ug, 2 times / day Route: oral Route: multiple Dose: 120 ug, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31119846/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/31119846/
Diarrhea	2.7%	120 ug 2 times / day multiple, oral Higher than recommended Dose: 120 ug, 2 times / day Route: oral Route: multiple Dose: 120 ug, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31119846/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/31119846/
Headache	8.7%	120 ug 2 times / day multiple, oral Higher than recommended Dose: 120 ug, 2 times / day Route: oral Route: multiple Dose: 120 ug, 2 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/31119846/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/31119846/
Nausea	3% Disc. AE	200 ug 4 times / day multiple, oral Higher than recommended Dose: 200 ug, 4 times / day Route: oral Route: multiple Dose: 200 ug, 4 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/12821234/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: FED Sources: https://pubmed.ncbi.nlm.nih.gov/12821234/

PubMed

Title	Date	PubMed
Efficacy of oral sildenafil in a beraprost-treated patient with severe pulmonary hypertension secondary to type I glycogen storage disease.	2009-10	19179780
Adaptive HNE-Nrf2-HO-1 pathway against oxidative stress is associated with acute gastric mucosal lesions.	2008-09	18617559
Beraprost sodium-induced hypotension in two patients after cardiac surgery.	2006-03	16607058
Amelioration by beraprost sodium, a prostacyclin analogue, of established renal dysfunction in rat glomerulonephritis model.	2002-08-02	12163121
Beraprost: a review of its pharmacology and therapeutic efficacy in the treatment of peripheral arterial disease and pulmonary arterial hypertension.	2002	11790158
Comparative effects of beraprost, a stable analogue of prostacyclin, with PGE(1), nitroglycerin and nifedipine on canine model of vasoconstrictive pulmonary hypertension.	2001-03	11334556
Prostacyclin analog prevents stress-induced expression of immediate early genes and gastric mucosal lesions in the rat stomach.	1999	10353594
Ligand binding specificities of the eight types and subtypes of the mouse prostanoid receptors expressed in Chinese hamster ovary cells.	1997-09	9313928
A dose-effect study of beraprost sodium in intermittent claudication.	1996-06	8761844
Clinical evaluation on combined administration of oral prostacyclin analogue beraprost and phosphodiesterase inhibitor cilostazol.	1995-02	7596955
Effect of beraprost sodium, a stable prostacyclin analogue, on pulmonary thromboembolism in mice.	1995-01-15	7740511
Protective effect of beraprost sodium, a new chemically stable prostacyclin analogue, against the deterioration of baroreceptor reflex following transient global cerebral ischaemia in dogs.	1990-01	2110014

Patents

Sample Use Guides

In Vivo Use Guide

Improvement of ulcers, pain & feeling of coldness associated with chronic arterial occlusion, Adult : 120 mcg daily in 3 divided doses. Primary pulmonary Hypertension: 60 mcg daily in 3 divided doses. Gradually increase dose if needed, up to a max of 180 mcg daily in 3-4 divided doses.

Route of Administration: Oral

In Vitro Use Guide

In suppressing platelet aggregation beraprost was especially potent with IC50 of 0.2-0.5 nM when platelets were activated by U46619, a thromboxane A2 analogue, or low concentrations of collagen which activates platelets through thromboxane A2 production. The IC50 values were 2-5 nM with ADP and epinephrine, which induce the formation of small aggregates independently of thromboxane A2 production.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 17:58:50 GMT 2025` Edited by `admin` on `Mon Mar 31 17:58:50 GMT 2025`
Record UNII	35E3NJJ4O6
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

TRK-100STP FREE ACID

Preferred Name

English

BERAPROST

Official Name

English

RAC-4-((1R,2R,3AS,8BS)-2-HYDROXY-1-((1E,3S,4RS)-3-HYDROXY-4-METHYLOCT-1-EN-6-YNYL)-2,3,3A,8B-TETRAHYDRO-1H-CYCLOPENTA(B)(1)BENZOFURAN-5-YL)BUTANOIC ACID

Common Name

English

(±)-(1R,2R,3AS,8BS)-2,3,3A,8B-TETRAHYDRO-2-HYDROXY-1-((E)-(3S,4RS)-3-HYDROXY-4-METHYL-1-OCTEN-6-YNYL)-1H-CYCLOPENTA(B)BENZOFURAN-5-BUTYRIC ACID

Common Name

English

beraprost [INN]

Common Name

English

1H-CYCLOPENTA(B)BENZOFURAN-5-BUTANOIC ACID, 2,3,3A,8B-TETRAHYDRO-2-HYDROXY-1-(3-HYDROXY-4-METHYL-1-OCTEN-6-YNYL)-

Common Name

English

Beraprost [WHO-DD]

Common Name

English

MDL-201229

Code

English

BERAPROST [USAN]

Common Name

English

BERAPROST [MI]

Common Name

English

ML-1229

Code

English

Classification Tree Code System Code

FDA ORPHAN DRUG

123099