Tolerability, Safety and Activity of a Muscle Relaxant Molecule IDN5243 in Patients With Low Back Pain

NCT02568826 | Withdrawn Phase 2

• 1 other identifier: XIL02/15
• Study Type: interventional
• Target: N/A
• Locations: 1 country
• Sites: 1

Brief Summary

This is a prospective cohort study, open-label, uncontrolled proof of concept trial. The trial objective is to evaluate the analgesic tolerability, safety and activity of IDN 5243 (3-glycosyl-3-O-demethylthiocolchicine derivative)administered intramuscularly at 4 mg b.i.d. for 5 days in the morning (8.00-10.00 AM) and in the evening (6.00-8.00 PM) in subjects with Low Back Pain (LBP).

Conditions

Low Back Pain

Keywords

Low Back Pain; Muscle relaxant

Outcome Measures

Primary Outcomes (2)

• Safety (vital signs, laboratory evaluations and incidence of adverse events)

  The primary outcome of the study will be to evaluate the systemic safety (vital signs, laboratory evaluations and incidence of adverse events) of the study drug assessed by Investigator taking into consideration the change from baseline to DAY 5.

  From baseline to day 5

• Local tolerability (4-point scale)

  Local tolerability assessed by the patient using a 4-point scale (where 0=none, 1=mild, 2=moderate, and 3=severe) every day during the treatment period and clinically by Investigator.

  From baseline to day 5

Secondary Outcomes (3)

• Analgesic activity (spontaneous pain) by Visual Analogue Scale

  From baseline to day 5

• Analgesic activity by Hand-To-Floor Distance (HTFD)

  On day 1 and 5

• Quality of Life by SF-36 questionnaire

  From baseline to day 5

Study Arms (1)

IDN 5243

EXPERIMENTAL

IDN 5243 is a new 3-glycosyl-3-Odemethylthiocolchicine derivative endowed with muscle-relaxant, anti-inflammatory and analgesic activities for intramuscular administration in 4 mg/mL vials. It will be administered twice daily for 5 consecutive days with the first administration in the morning (8.00-10.00 AM) and the second in the evening (6.00-8.00 PM).

Drug: 3-glycosyl-3-Odemethylthiocolchicine derivative

Interventions

3-glycosyl-3-Odemethylthiocolchicine derivative DRUG

IDN 5243 is a new muscle relaxant molecule. This molecule has showed significant anti-inflammatory activity by intraperitoneal route at 10 mg/kg in both carrageenan induced oedema and granuloma tests. IDN 5243 is a new 3-glycosyl-3-Odemethylthiocolchicine derivative endowed with muscle-relaxant, anti-inflammatory and analgesic activities. The primary packaging of test formulation will be a glass vial containing a solution of IDN 5243, 4 mg/ 1 mL. The secondary package will correspond to the patient's kit and will be a box containing ten (10) vials. The box label will be provided with a tear-off label.

Also known as: IDN 5243

IDN 5243

Eligibility Criteria

• Age: 18 Years - 70 Years
• Sex: all
• Healthy Volunteers: No
• Age Groups: Adult (18-64), Older Adult (65+)

You may qualify if:

• Male or female patients,
• years old inclusive,
• A diagnosis of LBP equal to or greater than 50 mm on VAS with severe or moderate lumbar muscle spasm naïve or in relapsing condition,
• Patients must have a medical history, physical and neurological examinations that support a clinical diagnosis of acute LBP that is felt down to the lower leg below the knee with the onset no longer than 30 days before Visit 1,
• Patients must be appropriate candidates for treatment with study medication in the Investigator's clinical judgment,
• Patients must be able to appropriately verbalize pain characteristics and to complete all protocol required measurements/assessments without assistance,
• Patients must be medically stable on the basis of physical examination, medical history, vital signs, and clinical laboratory tests performed at screening.

You may not qualify if:

• LPB of non-mechanical origin such as neoplasm, infection or inflammatory chronic disorder,
• Serum creatinine level \> 1.7 mg/dL or Urea \> 17 mmol/l,
• Severe to mild hepatic dysfunction,
• Abnormal blood count,
• Ascertained or presumptive hypersensitivity to the active principle and/or formulations' ingredients,
• History of anaphylaxis to drugs or allergic reactions in particular, history of hypersensitivity reactions (e.g. bronchospasm, rhinitis, urticaria) to drugs including to paracetamol,
• Patients with diabetic neuropathy, post-herpetic neuralgia, osteoarthritis pain, fibromyalgia,
• History of psychosis (e.g. schizophrenia or psychotic depression) or major depression (requiring treatment), diagnosis including dementia, anxiety, mental retardation; multiple sclerosis, Parkinson's Disease, Restless Legs Syndrome,
• Significant kidney or liver disease,
• History of gastrointestinal disorders,
• Blood coagulation disorders,
• Skin conditions affecting the site of application (e.g. eczema, weeping dermatitis),
• Pregnant or lactating women, or women of childbearing age not using a reliable method of contraception, or women of not child-bearing potential if not permanently sterilised or if not in post-menopausal status from at least two years,
• Males not to agree to use a reliable method of contraception during the study and the follow up period, if sexually active with a female of child-bearing potential,
• History of back (cervical, thoracic or lumbosacral) pain as 50% of the time in the 1 year prior to the first visit,

Sponsors & Collaborators

• Indena S.p.A: lead
• Sintesi Research Srl: collaborator

Study Sites (1)

Istituto di Reumatologia Complesso Integrato Columbus - Policlinico A. Gemelli

Rome, RM, 00168, Italy

Location

Related Publications (13)

• Chou R, Huffman LH; American Pain Society; American College of Physicians. Medications for acute and chronic low back pain: a review of the evidence for an American Pain Society/American College of Physicians clinical practice guideline. Ann Intern Med. 2007 Oct 2;147(7):505-14. doi: 10.7326/0003-4819-147-7-200710020-00008.

  PMID: 17909211 BACKGROUND

• Mellinghoff H. [Modern muscle relaxants and their clinical application]. Anaesthesist. 1994 Apr;43(4):270-82. doi: 10.1007/s001010050058. German.

  PMID: 8179178 BACKGROUND

• Bernstein E, Carey TS, Garrett JM. The use of muscle relaxant medications in acute low back pain. Spine (Phila Pa 1976). 2004 Jun 15;29(12):1346-51. doi: 10.1097/01.brs.0000128258.49781.74.

  PMID: 15187636 BACKGROUND

• Dillon C, Paulose-Ram R, Hirsch R, Gu Q. Skeletal muscle relaxant use in the United States: data from the Third National Health and Nutrition Examination Survey (NHANES III). Spine (Phila Pa 1976). 2004 Apr 15;29(8):892-6. doi: 10.1097/00007632-200404150-00014.

  PMID: 15082991 BACKGROUND

• Malanga GA, Dennis RL. Use of medications in the treatment of acute low back pain. Clin Occup Environ Med. 2006;5(3):643-53, vii. doi: 10.1016/j.coem.2006.03.002.

  PMID: 16963380 BACKGROUND

• Martin BI, Deyo RA, Mirza SK, Turner JA, Comstock BA, Hollingworth W, Sullivan SD. Expenditures and health status among adults with back and neck problems. JAMA. 2008 Feb 13;299(6):656-64. doi: 10.1001/jama.299.6.656.

  PMID: 18270354 BACKGROUND

• Wenig CM, Schmidt CO, Kohlmann T, Schweikert B. Costs of back pain in Germany. Eur J Pain. 2009 Mar;13(3):280-6. doi: 10.1016/j.ejpain.2008.04.005. Epub 2008 Jun 3.

  PMID: 18524652 BACKGROUND

• Gore M, Sadosky A, Stacey BR, Tai KS, Leslie D. The burden of chronic low back pain: clinical comorbidities, treatment patterns, and health care costs in usual care settings. Spine (Phila Pa 1976). 2012 May 15;37(11):E668-77. doi: 10.1097/BRS.0b013e318241e5de.

  PMID: 22146287 BACKGROUND

• Dagenais S, Caro J, Haldeman S. A systematic review of low back pain cost of illness studies in the United States and internationally. Spine J. 2008 Jan-Feb;8(1):8-20. doi: 10.1016/j.spinee.2007.10.005.

  PMID: 18164449 BACKGROUND

• Huskisson EC. Measurement of pain. Lancet. 1974 Nov 9;2(7889):1127-31. doi: 10.1016/s0140-6736(74)90884-8. No abstract available.

  PMID: 4139420 BACKGROUND

• Scott J, Huskisson EC. Graphic representation of pain. Pain. 1976 Jun;2(2):175-84. No abstract available.

  PMID: 1026900 BACKGROUND

• Williamson A, Hoggart B. Pain: a review of three commonly used pain rating scales. J Clin Nurs. 2005 Aug;14(7):798-804. doi: 10.1111/j.1365-2702.2005.01121.x.

  PMID: 16000093 BACKGROUND

• Carta M, Murru L, Botta P, Talani G, Sechi G, De Riu P, Sanna E, Biggio G. The muscle relaxant thiocolchicoside is an antagonist of GABAA receptor function in the central nervous system. Neuropharmacology. 2006 Sep;51(4):805-15. doi: 10.1016/j.neuropharm.2006.05.023. Epub 2006 Jun 30.

  PMID: 16806306 BACKGROUND

MeSH Terms

Conditions

Low Back Pain; Muscle Hypotonia

Condition Hierarchy (Ancestors)

Back Pain; Pain; Neurologic Manifestations; Signs and Symptoms; Pathological Conditions, Signs and Symptoms; Neuromuscular Manifestations; Nervous System Diseases

Study Officials

• Gianfranco Ferraccioli, MD

  Istituto di Reumatologia Complesso Integrato Columbus - Policlinico Gemelli Roma

  PRINCIPAL INVESTIGATOR

Study Design

• Study Type: interventional
• Phase: phase 2
• Allocation: NA
• Masking: NONE
• Purpose: OTHER
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: September 30, 2015
• First Posted: October 6, 2015
• Study Start: April 1, 2016
• Primary Completion: March 1, 2018
• Study Completion: March 1, 2018
• Last Updated: July 22, 2025

Record last verified: 2025-07

Locations

IT (1)