This is a multi-center, open-label study for eligible participants who were actively participating in the BPS-314d-MR-PAH-302 double-blind study (NCT01908699) at the time the study was concluded. This open-label extension (OLE) study will evaluate the safety, tolerability, and efficacy of long-term treatment with esuberaprost sodium tablets (Beraprost Sodium 314d Modified Release tablets).

Start Date10 Dec 2018

Sponsor / Collaborator

Lung Biotechnology PBC

NCT01966302 / CompletedPhase 2IIT

Compassionate Use of Beraprost Sodium 314d Modified Release (BPS-314d-MR) for Three Patients With Pulmonary Arterial Hypertension (PAH).

The purpose of this study is to see if Lung LLC's new experimental formulation of the medicine Beraprost Sodium, called Beraprost Sodium 314d Modified Release (BPS-314d-MR), can improve the symptoms of pulmonary arterial hypertension (PAH) in patients. An experimental drug is one that has not been approved by the U.S. Food and Drug Administration for use in the general public. This research study is for patients who have pulmonary arterial hypertension (PAH) and have just completed taking part in an earlier research study and received an older experimental formulation of Beraprost Sodium, called Beraprost Sodium Modified Release (BPS-MR). That earlier study was being done to see if BPS-MR could improve their PAH.
Patients may also be taking Tyvaso (treprostinil), Tracleer (bosentan), Letairis (ambrisentan), Adcirca (tadalafil) and/or Viagra or Revatio (sildenafil) to treat their PAH. The diagnosis of PAH means that the blood pressure in their lungs is higher than normal. The increased blood pressure in the lungs places a strain on the heart. The strain causes the heart to pump less blood into the lungs, causing shortness of breath and tiredness. The strain on the heart weakens the heart muscle making it less able to pump blood, a condition called heart failure. As heart failure develops, swelling in the feet and abdomen may occur.

Start Date01 Nov 2013

Sponsor / Collaborator

The Lundquist Institute

[+1]

JPRN-UMIN000006869 / RecruitingIIT

The study of effects of additional beraprost on the amelioration and retention of retinal and choroidal circulation after ranibizumab treatment in age-related macular degeneration. - The study of additional beraprost in age-related macular degeneration

Start Date01 Sep 2011

Sponsor / Collaborator

University of Nagasaki

100 Clinical Results associated with Esuberaprost Sodium

100 Translational Medicine associated with Esuberaprost Sodium

100 Patents (Medical) associated with Esuberaprost Sodium

Literatures (Medical) associated with Esuberaprost Sodium

01 Jun 2021·Clinical drug investigationQ4 · MEDICINE

Comparison of Pharmacokinetic Profiles of Beraprost Sustained Release in Japanese, Chinese, and Korean Healthy Adult Males

Q4 · MEDICINE

Article

Author: Sawamoto, Taiji ; Katashima, Masataka ; Shiramoto, Masanari ; Oikawa, Keishi ; Inaba, Masaki ; Inoue, Hiroshi ; Nakajo, Ikumi ; Kurumatani, Hajimu

BACKGROUND AND OBJECTIVES:

Beraprost sodium (BPS), an orally administrable prostaglandin I₂ derivative, is used for the treatment of chronic arterial occlusion and pulmonary arterial hypertension and has potential efficacy in nephropathy. Beraprost sustained release (beraprost SR) is an oral sustained-release formulation of BPS. To confirm the dose rationale reported in a multi-regional study of nephropathy patients in Asia, this open-label study evaluated ethnic differences in the pharmacokinetic profiles of BPS and its active diastereomer (BPS-314d) after beraprost SR administration among healthy Japanese, Chinese, and Korean adult males.

METHODS:

Twelve healthy subjects in each ethnic group were enrolled. Subjects received a single oral dose of 120 μg beraprost SR under fasting conditions.

RESULTS:

The geometric mean ratio (90% confidence interval) of the maximum plasma concentration (C_max) and area under the plasma concentration-time curve from time 0 to time of the last quantifiable concentration (AUC_last) of BPS was 1.12 (0.85-1.48) and 1.40 (1.05-1.86) in Chinese, and 1.18 (0.90-1.55) and 1.18 (0.89-1.58) in Korean compared to Japanese subjects. These differences were not clinically relevant. Similarly, differences in the C_max and AUC_last of BPS-314d were also small among the ethnic groups. Urinary excretion of BPS and BPS-314d was limited in all ethnic groups. Together, these findings indicate that the pharmacokinetics of beraprost SR are not affected by ethnic background.

CONCLUSIONS:

There were no clinically meaningful ethnic differences in the pharmacokinetics of BPS and BPS-314d following beraprost SR administration among Japanese, Chinese and Korean populations.

01 Aug 2019·Biochemical pharmacologyQ2 · MEDICINE

Pharmacology of the single isomer, esuberaprost (beraprost-314d) on pulmonary vascular tone, IP receptors and human smooth muscle proliferation in pulmonary hypertension

Q2 · MEDICINE

Article

Author: Whittle, Brendan J ; von Kessler, Kirby ; Moledina, Shahin ; Norel, Xavier ; Patel, Jigisha A ; Clapp, Lucie H ; Sista, Prakash ; Shen, Lei

BACKGROUND AND PURPOSE:

Beraprost is a prostacyclin analogue and IP receptor agonist which is approved to treat pulmonary arterial hypertension (PAH) in Asia. The beraprost-314d isomer (esuberaprost) is one of four stereoisomers contained within the racemic mixture of beraprost. The pharmacological profile of esuberaprost is now evaluated to determine how stereoisomer separation affects its potency and mode of action in functional assays.

EXPERIMENTAL APPROACH:

Vascular tone was assessed using wire myography in rat and human distal pulmonary arteries (PAs) pre-contracted with U46619 (100 nM). HEK-293 cells stably expressing the human IP receptor (HEK-293-IP) and pulmonary arterial smooth muscle cells (PASMCs) derived from PAH patients were used to assess cyclic AMP (cAMP) generation and cell proliferation, respectively.

KEY RESULTS:

Esuberaprost relaxed rat PAs with a 5-fold greater potency compared with beraprost, and effects were strongly inhibited by RO3244794 (IP receptor antagonist) or L-NAME (NO synthase inhibitor). Esuberaprost caused EP₃ receptor-dependent vasoconstriction at high concentrations ≥ 1000 nM, but contractions were 50% lower compared to beraprost. In HEK-293-IP cells, esuberaprost was 26-fold more potent (EC₅₀ 0.4 nM) at increasing cAMP than beraprost. In human PASMCs, esuberaprost was 40-fold more potent than beraprost at inhibiting cell proliferation (EC₅₀ 3 nM versus 120 nM), contrasting the 5-fold potency difference for cAMP elevation. Antiproliferative effects of esuberaprost appeared more dependent on NO than on the IP receptor. In PAs from patients with pulmonary hypertension, esuberaprost, caused some relaxation whereas beraprost instead produced a weak contraction.

CONCLUSIONS AND IMPLICATIONS:

Stereoisomer separation of beraprost has a significant effect on the pharmacology of the individual isomer, esuberaprost, identified in vitro as a highly potent prostanoid IP receptor agonist.

01 Nov 1993·Journal of cardiovascular pharmacologyQ4 · MEDICINE

Pharmacokinetics and Platelet Antiaggregating Effects of Beraprost, an Oral Stable Prostacyclin Analogue, in Healthy Volunteers

Q4 · MEDICINE

Article

Author: Jaillon, P. ; Demolis, J. L. ; Mouren, M. ; Funck-Brentano, C. ; Robert, A.

Beraprost sodium (BPS) is an orally stable analogue of prostacyclin that inhibits adenylate-cyclase-dependent platelet aggregation and is proposed for treatment of chronic arterial occlusion. To determine the duration and intensity of platelet antiaggregation with BPS, 12 healthy, nonsmoking, male white volunteers participated in a double-blind, dose-escalating design with randomized placebo, placebo-controlled, cross-over study. After overnight fasting, single (20, 40, 60 micrograms and placebo) and repeated [20, 40, 60 micrograms and placebo) and repeated [20, 40, 60 micrograms and placebo three times daily (t.i.d.) for 3 days] oral doses of BPS were administered. Mean percentage of inhibition of ADP-induced aggregation normalized to placebo was measured for 8 h after drug administration and related to plasma concentrations (Cp) of the active enantiomer (APS 314d). BPS 40 and 60 micrograms decreased platelet aggregation 1 h after single doses, and 0.5 h and 1 h after repeated doses. BPS 20 micrograms had no significant effect. APS 314d pharmacokinetics was linear, and its terminal half-life (t 1/2) ranged from 0.50 +/- 0.21 to 0.91 +/- 0.27 h (mean +/- SD) independently of BPS dose. Antiaggregating effects were poorly related to Cp of APS 314d (r2 < or = 0.2). Some subjects complained of moderate postdrug absorption headaches (7 of 12 after single and 8 of 12 after repeated doses) and flushes (6 of 12 and 7 of 12, respectively). These data indicate that orally active prostacyclin BPS (40 or 60 micrograms) exerts its maximal antiaggregating effects between 0.5 and 1 h.

News (Medical) associated with Esuberaprost Sodium

03 Mar 2021

·endpts.com

United axes PAH program Trevyent, once bought for cheap in acquisition of a rival, after FDA feedback

About three years after acquiring SteadyMed and its experimental pulmonary arterial hypertension drug Trevyent, United Therapeutics has decided to kick the program to the curb. In an 8-K form filed with the SEC on Tuesday, United revealed that they are shutting down development of Trevyent after receiving feedback from the FDA last week. The move marks the end of a long and bumpy road for the program, which had previously earned an RTF in 2017 and a CRL last April, as United moves forward with new Tyvaso formulations. Regulators had directed United to both redesign the Trevyent product and conduct an entirely new clinical study. That not only would have added significant delays to the program, United wrote, but may have proved unsuccessful in answering the FDA’s concerns. Specifically, the FDA took issue with the product’s pump device. Trevyent uses a pump to deliver a reformulated version of United’s mainstay PAH drug Remodulin. The accuracy of the pump, however, was not up to snuff in regulators’ eyes, and United said the agency wanted the company to improve the accuracy “in certain respects.” So United has decided to throw in the towel. They’re halting all development of the program after determining it wouldn’t be commercially reasonable to move forward. It marks an unceremonious end to a program they once picked up for a bargain from their competitors at SteadyMed in 2018. With the $216 million buyout, United had been looking to head off a PAH clash between the two companies by acquiring Trevyent itself. In addition to that program, SteadyMed at the time had been trying to invalidate one of United’s patents for the active ingredient in three of its prominent franchises: Remodulin, Tyvaso and Orenitram. Though United moved forward with Trevyent, submitting its NDA to US regulators in September 2019, the agency rejected its pitch in an April 2020 CRL. The FDA had said that some of the deficiencies previously pointed out had “not yet been addressed to its satisfaction,” United said at the time. United had been working on a new pitch and Tuesday’s decision stemmed from its subsequent meeting with the FDA to resubmit Trevyent for approval. It’s the latest in a couple of pipeline setbacks United has seen over the last few years. In 2019, the company dropped PAH hopeful esuberaprost after it failed a combo Phase III study, failing to show benefit when combined with Tyvaso over United’s older Remodulin drug. Then, in February, United revealed that a Phase II/III trial combining their Unituxin antibody with a standard treatment, irinotecan, failed to help small cell lung cancer patients live longer. United is instead moving forward with an inhaled reformulation of Tyvaso after snagging a priority review voucher from Y-mAbs Therapeutics last December for $105 million . The voucher had originally been slated for Y-mAbs’ application for Danyelza in neuroblastoma, and it wasn’t used for the FDA’s approval in November.

AntibodyPriority ReviewAcquisition

100 Deals associated with Esuberaprost Sodium

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KEGG	Wiki	ATC	Drug Bank
D10703	-	-	-

R&D Status

Approved

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Indication	Country/Location	Organization	Date
Occlusion of artery	KR	Jeil Pharmaceutical Co., Ltd.	17 Jan 1994
Pulmonary Arterial Hypertension	KR	Jeil Pharmaceutical Co., Ltd.	17 Jan 1994
Ulcer	KR	Jeil Pharmaceutical Co., Ltd.	17 Jan 1994

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Neoplasms	Phase 1	US	United Therapeutics Corp.	-

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03657095 (BPS-314d-MR-PAH-303 \| BEAT OLE, CTgov)	Phase 3	Pulmonary Arterial Hypertension	112	Esuberaprost (Esuberaprost)	foywedgpzz(hilnenawhb) = xfvignyndz vqgfzpkght (aynbkevifp, axamwtllzn - rclfuzxjsz) View more	-	07 Sep 2020
				Placebo+Esuberaprost (Placebo/Esuberaprost)	foywedgpzz(hilnenawhb) = ngqbkjbiql vqgfzpkght (aynbkevifp, kntcmzmjwp - isrhgbbcog) View more

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