Phase 1 Completed N=30 Randomized Other

OXN PR Tablet 5/2.5 mg and20/10 mg PK Study in Chinese Moderate to Severe Chronic Non-malignant Patients

Postoperative Pain

Source: ClinicalTrials.gov NCT02880475 ↗

Enrolled (actual)

Serious AEs

3.3%

Results posted

Jul 2019

Primary outcomePrimary: AUC0-48hr of Noroxycodone Plasma Concentration. — 81.72; 325.51 hr*ng/mL

Summary

This is an open-label, randomized, single-dose, parallel group study. The objectives of this study are to assess pharmacokinetics of oxycodone and naloxone from oxycodone/naloxone (OXN) prolonged release (PR) tablet 5/2.5 mg (OXN 5/2.5) and 20/10 mg (OXN 20/10) in Chinese patients with moderate to severe chronic non-malignant pain.

Outcome Measures

Outcome	Result	p-value
PRIMARY AUC0-48hr of Noroxycodone Plasma Concentration.	81.72; 325.51	—
PRIMARY AUC0-t of Noroxycodone Plasma Concentration	81.25; 325.37	—
PRIMARY AUC_%Extrap of Noroxycodone Plasma Concentration	2.99; 1.45	—
PRIMARY AUCinf of Noroxycodone Plasma Concentration	83.74; 330.44	—
PRIMARY Cmax of Noroxycodone Plasma Concentration	4.68; 20.69	—
PRIMARY Lambda_z of Noroxycodone Plasma Concentration	0.10; 0.10	—
PRIMARY T1/2 of Noroxycodone Plasma Concentration	7.42; 7.16	—
PRIMARY Tmax of Noroxycodone Plasma Concentration	4.50; 4.00	—
PRIMARY AUC0-48hr of Noroxymorphone Plasma Concentration	14.10; 65.84	—
PRIMARY AUC0-t of Noroxymorphone Plasma Concentration	12.92; 65.65	—
PRIMARY AUC_%Extrap of Noroxymorphone Plasma Concentration	14.89; 4.25	—
PRIMARY AUCinf of Noroxymorphone Plasma Concentration	15.76; 68.17	—
PRIMARY Cmax of Noroxymorphone Plasma Concentration	0.75; 3.54	—
PRIMARY Lambda_z of Noroxymorphone Plasma Concentration	0.08; 0.08	—
PRIMARY T1/2 of Noroxymorphone Plasma Concentration	8.55; 9.08	—
PRIMARY Tmax of Noroxymorphone Plasma Concentration	7.00; 5.00	—
PRIMARY AUC0-48hr of Oxycodone Plasma Concentration	89.48; 272.11	—
PRIMARY AUC0-t of Oxycodone Plasma Concentration	88.45; 271.21	—
PRIMARY AUC_%Extrap of Oxycodone Plasma Concentration	1.78; 0.57	—
PRIMARY AUCinf of Oxycodone Plasma Concentration	89.85; 272.71	—
PRIMARY Cmax of Oxycodone Plasma Concentration	6.69; 24.64	—
PRIMARY Lambda_z of Oxycodone Plasma Concentration	0.14; 0.14	—
PRIMARY T1/2 of Oxycodone Plasma Concentration	5.09; 5.03	—
PRIMARY Tmax of Oxycodone Plasma Concentration	3.75; 2.00	—
PRIMARY AUC0-48hr of Oxymorphone Plasma Concentration	3.70; 3.59	—
PRIMARY AUC0-t of Oxymorphone Plasma Concentration	0.14; 1.66	—
PRIMARY AUC_%Extrap of Oxymorphone Plasma Concentration	82.85; 51.11	—
PRIMARY AUCinf of Oxymorphone Plasma Concentration	—	—
PRIMARY Cmax of Oxymorphone Plasma Concentration	0.03; 0.30	—
PRIMARY Lambda_z of Oxymorphone Plasma Concentration	—	—
PRIMARY T1/2 of Oxymorphone Plasma Concentration	—	—
PRIMARY Tmax of Oxymorphone Plasma Concentration	0.75; 1.75	—
PRIMARY AUC0-48hr of 6-B-Naloxol Plasma Concentration	1655.48; 5065.33	—
PRIMARY AUC0-t of 6-B-Naloxol Plasma Concentration	1373.11; 5049.62	—
PRIMARY AUC_%Extrap of 6-B-Naloxol Plasma Concentration	21.24; 33.37	—
PRIMARY AUCinf of 6-B-Naloxol Plasma Concentration	1828.39	—
PRIMARY Cmax of 6-B-Naloxol Plasma Concentration	85.18; 269.53	—
PRIMARY Lambda_z of 6-B-Naloxol Plasma Concentration	0.07	—
PRIMARY T1/2 of 6-B-Naloxol Plasma Concentration	9.78	—
PRIMARY Tmax of 6-B-Naloxol Plasma Concentration	6.50; 1.75	—
PRIMARY AUC0-48hr of NLLG Plasma Concentration	57735.72; 209514.4	—
PRIMARY AUC0-t of NLLG Plasma Concentration	57737.49; 209514.4	—
PRIMARY AUC_%Extrap of NLLG Plasma Concentration	13.13; 20.07	—
PRIMARY AUCinf of NLLG Plasma Concentration	62953.71	—
PRIMARY Cmax of NLLG Plasma Concentration	3442.63; 11372.74	—
PRIMARY Lambda_z of NLLG Plasma Concentration	0.07	—
PRIMARY T1/2 of NLLG Plasma Concentration	11.32	—
PRIMARY Tmax of NLLG Plasma Concentration	11.00; 1.50	—
PRIMARY AUC0-48hr of NLXG Plasma Concentration	78725.81; 320734.4	—
PRIMARY AUC0-t of NLXG Plasma Concentration	77976.24; 320734.4	—
PRIMARY AUC_%Extrap of NLXG Plasma Concentration	1.56; 1.86	—
PRIMARY AUCinf of NLXG Plasma Concentration	79025.78; 326907.3	—
PRIMARY Cmax of NLXG Plasma Concentration	11488.62; 45789.83	—
PRIMARY Lambda_z of NLXG Plasma Concentration	0.14; 0.09	—
PRIMARY T1/2 of NLXG Plasma Concentration	5.28; 8.40	—
PRIMARY Tmax of NLXG Plasma Concentration	1.01; 1.25	—
PRIMARY AUC0-48hr of Naloxone Plasma Concentration	281.91; 650.42	—
PRIMARY AUC0-t of Naloxone Plasma Concentration	136.17; 443.88	—
PRIMARY AUC_%Extrap of Naloxone Plasma Concentration	47.82; 44.94	—
PRIMARY AUCinf of Naloxone Plasma Concentration	—	—
PRIMARY Cmax of Naloxone Plasma Concentration	33.21; 45.10	—
PRIMARY Lambda_z of Naloxone Plasma Concentration	—	—
PRIMARY T1/2 of Naloxone Plasma Concentration	—	—
PRIMARY Tmax of Naloxone Plasma Concentration	8.00; 1.00	—

Eligibility Criteria

Inclusion Criteria

Adult Chinese patients with moderate to severe chronic non-malignant pain.
Male and female subjects with age range 18 to 65 years (including 18 and 65), body weight ≥ 45kg and BMI range 18 to 30 (including 18 and 30).
Patients who should rate their pain (Pain Intensity Scale -"average pain" over the last 24 hours) as ≥4 on 0-10 scale.
Patients, who are able to read, understand and sign written informed consent prior to study participation and are willing to follow the protocol requirements.
Females of childbearing potential and less than one year post-menopausal must have a negative serum pregnancy test during screening visit and at check-in and be non-lactating. In addition, they must be willing to use adequate and reliable contraception throughout the study. Highly effective methods of birth control are defined as those which result in a low failure rate (i.e. less than 1% per year) when used consistently and correctly such as sterilization, implants, injectables, combined oral contraceptives, some IUDs (intrauterine Device, hormonal), sexual abstinence or vasectomised partner.

Exclusion Criteria

Females who are pregnant (positive β-human chorionic gonadotrophin [HCG] test) or lactating.
Use of opioid or opioid antagonist-containing medication in the 30 days before the start of the study.
Known sensitivity to oxycodone, naloxone, or related compounds.
Subjects with clinically unstable respiratory disease, dysfunction of the biliary tract, thyroid disease, adrenal cortical insufficiency, prostatic hypertrophy requiring intervention (medication or surgical) or renal artery stenosis, or any other medical condition, that, in the opinion of the investigator or the sub-investigator, precludes entry into this study.
Subject who have a past (within 5 years) history of malignant neoplasm including leukemia and lymphoma.
The electrocardiogram examination results are abnormal, in the opinion of the investigator or the sub-investigator, and are clinical significance.
Subjects with abnormal liver function (values exceed the upper limit of normal for AST, ALT or total bilirubin during the Screening Period) or abnormal renal function (values exceed the upper limit of normal for serum creatinine during the Screening Period).
Patients with a contraindication to the study medication.
Subjects who have a psychiatric disorder such that participation in the study may, in the opinion of the investigator or the sub-investigator, pose an unacceptable risk to the subject.
Subjects who have a current or past (within 5 years) history of substance or alcohol abuse, or subjects who give a positive result in drug abuse test during the Screening Period, or subjects who, in the opinion of the investigator or the sub-investigator, have demonstrated addictive or substance abuse behaviors.
Subjects with uncontrolled seizures or convulsive disorder.
Subjects who will receive any interventional therapy (surgery, paracentesis,etc) for arthritis during the study period.
History of or any current conditions that might have interfered with drug absorption, distribution, metabolism or excretion.
Any history of frequent nausea or emesis regardless of aetiology.
Participation in any clinical drug study during the 3 months preceding the initial dose in this study.
Use of any medication including vitamins, herbal and/or mineral supplements during the course of the study, other than Vitamin D, calcium supplements and continued use by females of contraceptive medication or HRT.
Consumption of alcoholic beverages within 48 hours before study drug administration, and refusal to abstain from alcohol until at least 48 hours after the last study drug administration.
Blood or blood products donated within 90 days prior to study drug administration or anytime during the study, except as required by this protocol.
Positive results of urine drug screen(for opioids, barbiturate

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Data sourced from ClinicalTrials.gov (NCT02880475). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.