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Trade names | Ecclock |
Other names | BBI 4000 |
Routes of administration | Topical gel |
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Formula | C22H32BrNO5 |
Molar mass | 470.404 g·mol−1 |
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Sofpironium bromide (trade name Ecclock; development code BBI-4000) is a drug used to treat hyperhidrosis (excessive sweating). It was approved in Japan in 2020 as a 5% gel for the treatment of primary axillary hyperhidrosis (PAH). [1] [2] [3]
Sofpironium bromide is an anticholinergic agent that reduces sweating by inhibiting M3 muscarinic receptors in eccrine glands. [3] It is a retrometabolically-designed drug (or "soft drug") based on glycopyrronium bromide, [4] [5] meaning it has been designed to exert the desired effects at the site of administration, after which it is quickly converted into an inactive non-toxic metabolite upon entering systemic circulation avoiding the typical anticholinergic side-effects caused by off-site action.
Sofpironium bromide was discovered at Bodor Laboratories by Nicholas Bodor and licensed to Botanix SB, a subsidiary of Botanix Pharmaceuticals. This license was previously owned by Fresh Tracks Therapeutics, which was then sold to Botanix in 2022, exclusively in the field of hyperhidrosis, with all other uses having been retained by Bodor Laboratories. Additional sublicenses were executed with Kaken Pharmaceutical and Dong Wha Pharmaceutical.
Benzatropine (INN), known as benztropine in the United States and Japan, is a medication used to treat movement disorders like parkinsonism and dystonia, as well as extrapyramidal side effects of antipsychotics, including akathisia. It is not useful for tardive dyskinesia. It is taken by mouth or by injection into a vein or muscle. Benefits are seen within two hours and last for up to ten hours.
Anticholinergics are substances that block the action of the acetylcholine (ACh) neurotransmitter at synapses in the central and peripheral nervous system.
Iontophoresis is a process of transdermal drug delivery by use of a voltage gradient on the skin. Molecules are transported across the stratum corneum by electrophoresis and electroosmosis and the electric field can also increase the permeability of the skin. These phenomena, directly and indirectly, constitute active transport of matter due to an applied electric current. The transport is measured in units of chemical flux, commonly μmol/(cm2*hour). Iontophoresis has experimental, therapeutic and diagnostic applications.
Ipratropium bromide, sold under the trade name Atrovent among others, is a type of anticholinergic medication which opens up the medium and large airways in the lungs. It is used to treat the symptoms of chronic obstructive pulmonary disease and asthma. It is used by inhaler or nebulizer. Onset of action is typically within 15 to 30 minutes and lasts for three to five hours.
Hyperhidrosis is a condition characterized by abnormally increased sweating, in excess of that required for regulation of body temperature. Although primarily a benign physical burden, hyperhidrosis can deteriorate quality of life from a psychological, emotional, and social perspective. In fact, hyperhidrosis almost always leads to psychological as well as physical and social consequences. People suffering from it present difficulties in the professional field, more than 80% experiencing a moderate to severe emotional impact from the disease and half are subject to depression.
Papaverine is an opium alkaloid antispasmodic drug, used primarily in the treatment of visceral spasms and vasospasms, occasionally in the treatment of erectile dysfunction and acute mesenteric ischemia. While it is found in the opium poppy, papaverine differs in both structure and pharmacological action from the analgesic morphine and its derivatives.
Glycopyrronium bromide is a medication of the muscarinic anticholinergic group. It does not cross the blood–brain barrier and consequently has few to no central effects. It is given by mouth, via intravenous injection, on the skin, and via inhalation. It is a synthetic quaternary ammonium compound. The cation, which is the active moiety, is called glycopyrronium (INN) or glycopyrrolate (USAN).
Beta2-adrenergic agonists, also known as adrenergic β2 receptor agonists, are a class of drugs that act on the β2 adrenergic receptor. Like other β adrenergic agonists, they cause smooth muscle relaxation. β2 adrenergic agonists' effects on smooth muscle cause dilation of bronchial passages, vasodilation in muscle and liver, relaxation of uterine muscle, and release of insulin. They are primarily used to treat asthma and other pulmonary disorders. Bronchodilators are considered an important treatment regime for Chronic obstructive pulmonary disease (COPD) and are usually used in combination with short acting medications and long acting medications in a combined inhaler.
Zimelidine was one of the first selective serotonin reuptake inhibitor (SSRI) antidepressants to be marketed. It is a pyridylallylamine, and is structurally different from other antidepressants.
Oxybutynin, sold as under the brand names Ditropan among others, is a medication used to treat overactive bladder. It works similar to tolterodine, darifenacin, and solifenacin. While used for bed wetting in children, evidence to support this use is poor. It is taken by mouth or applied to the skin.
Cyproheptadine, sold under the brand name Periactin among others, is a first-generation antihistamine with additional anticholinergic, antiserotonergic, and local anesthetic properties.
Loteprednol is a topical corticosteroid used to treat inflammations of the eye. It is marketed by Bausch and Lomb as Lotemax and Loterex.
Iloperidone, commonly known as Fanapt and previously known as Zomaril, is an atypical antipsychotic for the treatment of schizophrenia.
Bornaprine is a synthetic anticholinergic medication that is primarily used to treat Parkinson's disease. Additionally, bornaprine has been used to treat other disorders, including hyperhidrosis.
Bromazine, sold under the brand names Ambodryl, Ambrodil, and Deserol among others, also known as bromodiphenhydramine, is an antihistamine and anticholinergic medication of the ethanolamine class. It is an analogue of diphenhydramine with a bromine substitution on one of the phenyl rings.
Amitriptylinoxide, or amitriptyline N-oxide, is a tricyclic antidepressant (TCA) which was introduced in Europe in the 1970s for the treatment of depression.
Imipraminoxide, or imipramine N-oxide, is a tricyclic antidepressant (TCA) that was introduced in Europe in the 1960s for the treatment of depression.
Focal hyperhidrosis, also known as primary hyperhidrosis, is a disease characterized by an excessive sweating localized in certain body regions. Studies suggest that this condition, affecting between 1% and 3% of the US population, seems to have a genetic predisposition in about two thirds of those affected.
Aluminum chloride hexahydrate, sold under the brand name Hydrosal Gel among others, is a first-line treatment for excessive sweating.
In the field of drug discovery, retrometabolic drug design is a strategy for the design of safer drugs either using predictable metabolism to an inactive moiety or using targeted drug delivery approaches. The phrase retrometabolic drug design was coined by Nicholas Bodor. The method is analogous to retrosynthetic analysis where the synthesis of a target molecule is planned backwards. In retrometabolic drug design, metabolic reaction information of drugs is used to design parent drugs whose metabolism and distribution can be controlled to target and eliminate the drug to increase efficacy and minimize undesirable side effects. The new drugs thus designed achieve selective organ and/or therapeutic site drug targeting and produce safe therapeutic agents and safe environmental chemicals. These approaches represent systematic methodologies that thoroughly integrate structure-activity (SAR) and structure-metabolism (SMR) relationships and are aimed at designing safe, locally active compounds with improved therapeutic index.