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Last update 23 Jan 2025

PDE1 x PDE4

Last update 23 Jan 2025

Basic Info

Related Targets

PDE1PDE4

Drugs associated with PDE1 x PDE4

GPD-1116

Target

MMP12 x PDE1 x PDE4

Mechanism

MMP12 inhibitors [+2]

Active Org.-

Originator Org.

ASKA Pharmaceutical Co., Ltd.

Active Indication-

Inactive Indication

Allergic asthma [+2]

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

LASSBio-985

Target

PDE1 x PDE4

Mechanism

PDE1 inhibitors [+1]

Active Org.-

Originator Org.

Federal University of Rio de Janeiro

Active Indication-

Inactive Indication

Hypertension

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

KF-19514

Target

PDE1 x PDE4

Mechanism

PDE1 inhibitors [+1]

Active Org.-

Originator Org.

Kyowa Kirin Co., Ltd.

Active Indication-

Inactive Indication

Asthma [+2]

Drug Highest PhasePending

First Approval Ctry. / Loc.-

First Approval Date20 Jan 1800

Clinical Trials associated with PDE1 x PDE4

EUCTR2008-005813-23-GB

/ Not yet recruitingNot Applicable

Phase IIa study to evaluate the effects of GPD-1116 on late phase asthmatic response to allergen challenge in asthmatic patients.

Start Date24 Dec 2008

Sponsor / Collaborator

ASKA Pharmaceutical Co., Ltd.

100 Clinical Results associated with PDE1 x PDE4

100 Translational Medicine associated with PDE1 x PDE4

0 Patents (Medical) associated with PDE1 x PDE4

175

Literatures (Medical) associated with PDE1 x PDE4

26 Dec 2024·Journal of Medicinal Chemistry

Discovery and Optimization of Dihydroquinolin-2(1H)-ones as Novel Highly Selective and Orally Bioavailable Phosphodiesterase 5 Inhibitors for the Treatment of Pulmonary Arterial Hypertension

Article

Author: Zhang, Bei ; Chen, Jun-Wei ; Wang, Gang ; Zhao, Pei-Liang ; Cai, Jian-Fan ; Tan, Wen-Ming ; Zou, Zhong-Kai ; Li, Wei-En ; Wu, Wei-Pei ; Liang, Jing-Nan ; Ruan, Xiao-Hong

Phosphodiesterase 5 (PDE5) is a cGMP-specific hydrolytic enzyme and widely distributed in versatile tissues. PDE5 has been identified as a valid therapeutic target for treating erectile dysfunction and pulmonary arterial hypertension (PAH). Herein, a hit-to-lead structural optimizations were performed on the PDE1 inhibitor 10c, leading to compound 14b possessing great potency against PDE5A (IC₅₀ = 3 nM) with high selectivity over PDE1, PDE2, PDE3, PDE4, PDE7, PDE8, PDE9, PDE10, and PDE11 by more than 1125-fold, and remarkable safety properties. Furthermore, oral administration of 14b (5.0 mg/kg) exerted much better pharmacodynamics effects on both mPAP (mean pulmonary artery pressure) and RVHI (index of right ventricle hypertrophy) than sildenafil citrate (10.0 mg/kg) in a monocrotaline-induced PAH rat model. Overall, these results proposed a novel highly selective PDE5 inhibitor 14b which could serve as a potential candidate for treatment of PAH.

01 Oct 2024·Biophysical Chemistry

Computational and in vitro binding studies of theophylline against phosphodiesterases functioning in sperm in presence and absence of pentoxifylline

Article

Author: Rajakumara, Eerappa ; Abhishek, Suman ; Dey, Sreenath ; Nitin, Kulhar ; Raj, Gupta

Fertility is a result of a synergy among the sperm's various functions including capacitation, motility, chemotaxis, acrosome reaction, and, finally, the fertilization of the oocyte. Subpar motility is the most common cause of infertility in males. Cyclic adenosine monophosphate (cAMP) signalling underlies motility and is depleted by the phosphodiesterases (PDEs) in sperm, such as PDE10A, PDE1, and PDE4. Therefore, the PDE inhibitor (PDEI) category of fertility drugs aim to enhance motility in assisted reproduction technologies (ARTs) through inhibition of PDEs, though they might have adverse effects on other physiological variables. For example, the popular drug pentoxifylline (PTX), widely used in ARTs, improves motility but causes premature acrosome reaction and exerts toxicity on the fertilized oocyte. Another xanthine-derived drug, theophylline (TP), has been repurposed for treating infertility, but its mechanism of PDE inhibition remains unexplored. Here, using biophysical and computational approaches, we identified that TP binds to the same binding pocket as PTX with higher affinity than PTX. We also found that PTX and TP co-bind to the same binding pocket, but at different sites.

01 Jun 2024·médecine/sciences

Les phosphodiestérases des nucléotides cycliques

Review

Author: Leroy, Jérôme ; Fischmeister, Rodolphe ; Kamel, Rima ; Barthou, Aurélien ; Vandecasteele, Grégoire

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