CAS No. : 863513-91-1

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Cat No:I005180
Molecular Formula:C24H27FN2O
Molecular Weight:378.48
Target:Opioid Receptor
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Appearance:Solid powder
Purity: > 98%
Cat No:I005180
Cas No:863513-91-1

Cebranopadol(GRT-6005) is a novel first in class compounds with potent agonist activity on ORL-1 (opioid receptor like -1) and the well established mu opioid receptor. Cebranopadol and GRT 6006 are novel first-in-class compounds with unique pharmacological and pharmacokinetic profiles that may enhance their effect in certain pain conditions. The unique mode of action of these compounds builds on the ORL-1 receptor and, supported by the established mu opioid receptor, is particularly suitable for the treatment of moderate to severe chronic pain.

1. Eur J Pain. 2018 Oct 26. doi: 10.1002/ejp.1331. [Epub ahead of print]
Cancer-related chronic pain: investigation of the novel analgesic drug candidate cebranopadol in a randomized, double-blind, non-inferiority trial.
Eerdekens MH(1), Kapanadze S(1), Koch ED(1), Kralidis G(1), Volkers G(1), Ahmedzai SH(2), Meissner W(3).
Author information:
(1)Grünenthal GmbH, Aachen, Germany. (2)Department of Oncology, University of Sheffield, Sheffield, United Kingdom. (3)Department of Palliative Care, Jena University Hospital, Jena, Germany.
BACKGROUND: Cancer-related pain is a growing health problem given the increasing life expectancy of cancer patients. Opioids are commonly used to treat cancer-related pain, but carry the risk of severe side effects, limiting their use. Cebranopadol is a first-in-class drug candidate, combining nociceptin/orphanin FQ peptide and opioid peptide receptor agonism. This trial examined the analgesic efficacy of cebranopadol compared with morphine prolonged release (PR) in patients with moderate to severe cancer-related pain. METHODS: This double-blind, parallel-group, multiple-dose trial was designed as non-inferiority trial for efficacy of cebranopadol versus morphine PR. Planned with 524 patients, finally 126 patients were treated for up to 7 weeks (low accrual). The primary efficacy endpoint was the average amount of daily rescue medication intake (morphine immediate release) over the last 2 weeks of treatment.
RESULTS: For the primary endpoint, non-inferiority of cebranopadol with and superiority over morphine PR were demonstrated (Full Analysis Set: ∆[95%CI]=-7.48 mg [-12.05, -2.92]; Per Protocol Set: ∆[95%CI]=-4.67 mg [-9.25, -0.10]). The vast majority of patients (≥75%, either treatment) had clinically relevant pain reduction, non-inferiority on this secondary endpoint was not shown. Mostly used doses were ≤800 μg cebranopadol or ≤120 mg morphine PR daily. A total of 83.1% of patients on cebranopadol and 82.0% on morphine PR experienced treatment-emergent adverse events.
CONCLUSIONS: Cebranopadol was effective, safe, and well tolerated in the dose range tested (200 to 1,000 μg) in patients suffering from chronic moderate to severe cancer-related pain and was superior to morphine PR on the primary endpoint. This article is protected by copyright. All rights reserved.

2. Clin Pharmacokinet. 2018 Jan;57(1):31-50. doi: 10.1007/s40262-017-0545-1.
Clinical Pharmacokinetic Characteristics of Cebranopadol, a Novel First-in-Class Analgesic.
Kleideiter E(1), Piana C(2), Wang S(2), Nemeth R(3), Gautrois M(4). Author information:
(1)Data Sciences-Clinical Pharmacology, Grünenthal GmbH, Zieglerstrasse 6, 52078, Aachen, Germany. (2)Data Sciences-Pharmacometrics, Grünenthal GmbH, Aachen, Germany. (3)Data Sciences-Biostatistics, Grünenthal GmbH, Aachen, Germany. (4)Preclinical Drug Development-Pharmacokinetics, Grünenthal GmbH, Aachen, Germany.
Erratum in
Clin Pharmacokinet. 2018 Aug;57(8):1057-1058.
BACKGROUND AND OBJECTIVES: Cebranopadol is a novel first-in-class analgesic acting as a nociceptin/orphanin FQ peptide and opioid peptide receptor agonist with central analgesic activity. It is currently in clinical development for the treatment of chronic pain conditions. This trial focuses on the clinical pharmacokinetic (PK) properties of cebranopadol after oral single- and multiple-dose administration.
METHODS: The basic PK properties of cebranopadol were assessed by means of noncompartmental methods in six phase I clinical trials in healthy subjects and patients. A population PK analysis included two further phase I and six phase II clinical trials.
RESULTS: After oral administration of the immediate-release (IR) formulation, cebranopadol is characterized by a late time to reach maximum plasma concentration [C max] (4-6 h), a long half-value duration [HVD] (14-15 h), and a terminal phase half-life in the range of 62-96 h. After multiple once-daily dosing in patients, an operational half-life (the dosing interval resulting in an accumulation factor [AF] of 2) of 24 h was found to be the relevant factor to describe the multiple-dose PKs of cebranopadol. The time to reach steady state was approximately 2 weeks, the AF was approximately 2, and peak-trough fluctuation (PTF) was low (70-80%). Dose proportionality at steady state was shown for a broad dose range of cebranopadol 200-1600 µg. A two-compartment disposition model with two lagged transition compartments and a first-order elimination process best describes cebranopadol data in healthy subjects and patients after single- and multiple-dose administration.
CONCLUSIONS: Cebranopadol formulated as an IR product can be used as a once-daily formulation; it reaches C max after only 4-6 h, and has a long HVD and a low PTF. Therefore, from a PK perspective, cebranopadol is an attractive treatment option for patients with chronic pain.

3. J Clin Pharm Ther. 2017 Feb;42(1):8-17. doi: 10.1111/jcpt.12461. Epub 2016 Oct 24.
Cebranopadol: novel dual opioid/NOP receptor agonist analgesic.
Raffa RB(1)(2), Burdge G(1), Gambrah J(1), Kinecki HE(1), Lin F(1), Lu B(1), Nguyen JT(1), Phan V(1), Ruan A(1), Sesay MA(1), Watkins TN(1).
Author information:
(1)Temple University School of Pharmacy, Philadelphia, PA, USA. (2)University of Arizona College of Pharmacy, Tucson, AZ, USA.
WHAT IS KNOWN AND OBJECTIVE: Chronic pain presents a difficult clinical challenge because of the limited efficacy, the limiting adverse-effect profile or the abuse potential of current analgesic options. Cebranopadol is a novel new agent in clinical trials that combines dual agonist action at opioid and nociceptin/orphanin FQ peptide (NOP) receptors. It is the first truly unique, centrally acting analgesic in several years. We here review the basic and clinical pharmacology of cebranopadol.
METHODS: Published literature and Internet sources were searched to identify information related to the basic science (pharmacology and medicinal chemistry) and development (clinical trial) information on the mechanism of dual opioid and NOP receptor pharmacologic action in general, and for cebranopadol in particular. The identified sources were reviewed and the information synthesized.
RESULTS: The preclinical testing of cebranopadol has characterized it as a dual opioid and NOP receptor agonist that displays antinociceptive and antihyperalgesic action in a variety of acute and chronic pain models in animals. Unlike most current traditional opioids, it is generally more potent against neuropathic than nociceptive pain. Several phase 2 clinical trials have been completed.
WHAT IS NEW AND CONCLUSION: Despite the medical need, a truly novel centrally acting analgesic has not been developed in many years. Cebranopadol represents a truly novel mechanistic approach. Its actual place in pain pharmacotherapy awaits the results of phase 3 clinical trials.
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