access-principles-1access-principles-2access-principles-3backcarrierdevelopmentease_of_administrationexportimplantableinjectablenon-implantablenon_carriernon_injectableother_featuresprintroute_of_administrationtherapeutic_areatype_of_tech

Drug information

Drug's link(s)

Not provided

Generic name

Ivermectin

Brand names

Not provided

Compound type

Small molecule

Drug class/category

Not provided

Summary

Ivermectin is a broad-spectrum anthelmintic that possesses significant potential as a first-in-class endectocide providing vector-based malaria control. Ivermectin functions by binding glutamate-gated chloride channels present in parasital nerve and muscle cells, which results in the elimination of the organism. An extended-release oral ivermectin formulation known as LYN-163 is currently being developed by Lyndra Therapeutics and is undergoing phase I clinical trials. This ultra-long acting, oral drug delivery system is based on their proprietary LYNX™ technology which supports once fortnightly dosing. Other long-acting ivermectin formulations are in the pre-clinical phase and include a polymer-based injectable developed by MedinCell utilising their proprietary BEPO® drug delivery system.

Approval status

Unknown

Regulatory authorities

Unknown

Therapeutic area(s)

  • Malaria
  • COVID 19
  • Other(s) : "other parasitic infections"
Use case(s)
  • Pre-Exposure Prophylaxis (PrEP)
  • Post-Exposure Prophylaxis (PEP)
  • Treatment

Administration route

Oral, Subcutaneous

Associated long-acting platforms

Oral solid form, Polymer-based particles

Use of drug

Ease of administration
  • Administered by a nurse
  • Administered by a specialty health worker
  • Self-administered
  • To be determined
Frequency of administration

Not provided

User acceptance
Not provided

Dosage

Available dose and strength

Not provided

Maximum dose

Not provided

Recommended dosing regimen

Not provided

Additional comments

Not provided

Dosage link(s)

Not provided

Associated compounds, formulations and regimens

Not provided

Associated technologies

Compare
BEPO®
LYNX

Additional information

Not provided

Developer(s)

Merck / MSD
Originator
International

Merck / MSD

Dr. William C. Campbell conducted his co-recipient 2015 Physiology or Medicine Nobel Prize-winning Work at Merck Research Laboratories. He received the prize with Satoshi Omura for the discovery of avermectin which led to Merck’s development of ivermectin, to treat river blindness. They share the prize with Youyou Tu for her discoveries concerning a novel therapy against malaria.

Various generic manufacturers
Generic
international

Various generic manufacturers

Ivermectin 3mg manufactured buy generic manufactures including: ARROW LAB, BIOGARAN, CRISTERS, EG, EG LABO, PIERRE FABRE, SANDOZ, SIGILLATA, SUBSTIPHARM, TEVA, VIATRIS, ZENTIVA, Taj Pharmaceuticals, Dr. Reddy's labs.

Drug structure

Scale-up and manufacturing prospects

Scale-up prospects

Compound is commercially manufactured.

Tentative equipment list for manufacturing

(1) Fermentation & Extraction tanks: Bacterial fermentation vessels to produce avermectin and its subsequent extraction from the fermentation broth. (2) Hydrogenation reactors: Allows the conversion of avermectin to ivermectin by selective hydrogenation. (3) Filtration systems: Removes impurities from the ivermectin solution. (4) Crystallizers: Vessels used to crystallize ivermectin from the solution. (5) Dryers: Required to remove solvent from the crystallized ivermectin. (6) Packaging equipment: Machinery to package the final drug product.

Manufacturing

Avermectin derivatives such as ivermectin are unstable in acidic and alkaline conditions, in addition to being sensitive to strong light. Product formulations containing avermectins usually include antioxidant excipients as they susceptible to chemical oxidation processes.

Specific analytical instrument required for characterization of formulation

(1) Identification of residual impurities: High-performance liquid chromatography (HPLC), gas chromatography (GC), mass spectrometry (MS). (2) Determine concentration: Ultraviolet-visible spectrophotometry. (3) Elucidate melting point and identify polymorphic forms: Differential scanning calorimetry. (4) Analyse crystal structure and determine polymorphic forms: X-ray powder diffraction (XRPD). (5) Drug solubility: Dissolution testing apparatus.

Excipients & delivery device(s)

Proprietary excipients used

Not provided

Novel excipients or existing excipients at a concentration above Inactive Ingredient Database (IID) for the specified route of administration

Not provided

Residual solvents used

Not provided

Delivery device(s)

Lyndra’s proprietary LYNX™ drug delivery platform is a novel approach to oral drug delivery that enables once-a-week or even once-a-month dosing. Key proprietary features include: (1) A flexible core that allows the dosage form to maintain its desired shape in the stomach, preventing premature passage into the small intestine. (2) Linkers connecting dosage form arms to the core. These linkers are designed to soften and disintegrate, allowing the dosage form to safely exit the body. (3) A proprietary coating that makes the capsule easy to swallow and ensures it remains intact in the oesophagus.

Safety, Efficacy and Evidence Summary

Safety

Not provided

Efficacy

Not provided

Evidence Summary

Not provided

References and relevant studies

Not provided

Description

Long-acting injectable ivermectin formulation

Brief description

This invention relates to novel, long-acting injectable formulations. These formulations comprise: (a) a therapeutic agent selected from the group consisting of, e.g., insecticides, acaricides, parasiticides, growth enhancers and oil-soluble NASIDS; (b) hydrogenated castor oil and (c) a hydrophobic carrier comprising: (i) triacetin, benzyl benzoate or ethyl oleate or a combination thereof; and (ii) acylated monoglycerides, propyl dicaprylates/dicaprates or caprylic/capric acid triglycerides or a combination thereof. Also provided herein is a method for the treatment or prevention of various disease states by the parental administration of the invention formulations.

Representative patent

WO1999027906

Category

Formulation

Patent holder

Merck Sharp & Dohme Corp; Merial LLS (acquired by BI)

Exclusivity

Long-acting injectable parasiticide formulation of specific excipients and therapeutic agent such as ivermectin, for various use including the prevention and treatment of parasitic infestation

Expiration date

September 14, 2018

Status

Expired

Description

Ivermectin compound

Brief description

Derivatives of C-076 are described in which the C-076 molecule, as series of macrolides, has a specific unsaturation, at the 22,23-position, catalytically reduced. Further reaction of the reduced C-076 compounds are also possible. The compounds thus produced have profound anthelmintic, insecticidal, ectoparasiticidal and acaracidal activity. Compositions containing the described C-076 derivatives as the active ingredient thereof are also disclosed.

Representative patent

US4199569

Category

Compound

Patent holder

Merck & Co, Inc.

Exclusivity

Not provided

Expiration date

April 22, 1997

Status

Expired