U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Status:
First marketed in 0652
Source:
alcohol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alcohols exhibit rapid broad-spectrum antimicrobial activity against vegetative bacteria (including mycobacteria), viruses, and fungi but are not sporicidal. They are, however, known to inhibit sporulation and spore germination, but this effect is reversible. Because of the lack of sporicidal activity, alcohols are not recommended for sterilization but are widely used for both hard-surface disinfection and skin antisepsis. Lower concentrations may also be used as preservatives and to potentiate the activity of other biocides. Many alcohol products include low levels of other biocides (in particular chlorhexidine), which remain on the skin following evaporation of the alcohol, or excipients (including emollients), which decrease the evaporation time of the alcohol and can significantly increase product efficacy. Ethanol in combination with: chlorhexidine gluconate 1% was approved to use in surgical hand antiseptic. It significantly reduces the number of microorganisms on the hands and forearms prior to surgery or patient care. Ethanol is also used as a co-solvent to dissolve many insoluble drugs and to serve as a mild sedative in some medicinal formulations. Ethanol is metabolized by the hepatic enzyme alcohol dehydrogenase. Ethanol affects the brain’s neurons in several ways. It alters their membranes as well as their ion channels, enzymes, and receptors. Alcohol also binds directly to the receptors for acetylcholine, serotonin, GABA, and the NMDA receptors for glutamate. The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). It also inhibits NMDA receptor functioning. In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes.

Class (Stereo):
CHEMICAL (ACHIRAL)

Isopropanolamine (1-Amino-2-propanol) is a colorless to yellowish liquid with an amine-like odor. It is miscible in water. Intermediate used in the production of dyes, lubrification oils, corrosion inhibitor, detergents, cutting fluids.
Status:
US Approved OTC
Source:
21 CFR 346.10(b) anorectal:local anesthetic benzyl alcohol
Source URL:
First marketed in 1921

Class (Stereo):
CHEMICAL (ACHIRAL)


Benzyl Alcohol is an aromatic alcohol used in a wide variety of cosmetic formulations as a fragrance component, preservative, solvent, and viscosity-decreasing agent. FDA agency approved benzyl alcohol for the treatment of head lice. The drug acts on head lice by inhibiting them from closing their respiratory spiracles, allowing the vehicle to obstruct the spiracles and causing the lice to asphyxiate.
Status:
Investigational
Source:
NCT00352729: Not Applicable Interventional Withdrawn Burns
(2006)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT01607385: Phase 1 Interventional Completed Diabetes Mellitus, Type 2
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

GSK-1614235 (mizagliflozin) is a sodium glucose co-transporter type 1 (SGLT1) inhibitor that has been investigated for treatment in type 2 diabetes. It is thought to suppress glucose absorption from the intestine in a way that is different from conventional type 2 diabetes drugs, thereby improving postprandial hyperglycemia. Phase 1 studies have been completed.
Status:
Investigational
Source:
NCT02357888: Phase 2 Interventional Completed Healthy Highly Dependant Smokers
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Vanillyl alcohol is a monomethoxybenzene that is 2-methoxyphenol substituted by a hydroxymethyl group at position 4. It has a role as a plant metabolite. It is a member of guaiacols and a member of benzyl alcohols. Vanillyl alcohol is a phenolic alcohol and is used as a flavoring agent in foods and beverages. Vanillyl alcohol effectively inhibited the cytotoxicity and improved cell viability in MPP+-induced MN9D dopaminergic cells. Vanillyl alcohol attenuated the elevation of reactive oxygen species (ROS) levels, decreased in the Bax/Bcl-2 ratio and poly (ADP-ribose) polymerase proteolysis. These results indicate that vanillyl alcohol protected dopaminergic MN9D cells against MPP+-induced apoptosis by relieving oxidative stress and modulating the apoptotic process and is therefore a potential candidate for treatment of neurodegenerative diseases such as Parkinson's disease.
Status:
Investigational
Source:
NCT00608634: Phase 2 Interventional Completed Precancerous Condition
(2004)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



The monoterpene perillyl alcohol (POH) is a naturally occurring compound derived from citrus fruits, mint, and herbs. It exhibited chemotherapeutic potential against various malignant tumors in preclinical models and was being tested in clinical trials in patients with refractory advanced cancers. POH was formulated in soft gelatine capsules and orally administered to cancer patients several times a day on a continuous basis. However, such clinical trials in humans yielded disappointing results, also because of the large number of capsules that had to be swallowed caused hard-to-tolerate intestinal side effects, causing many patients to withdraw from treatment due to unrelenting nausea, fatigue, and vomiting. The clinical trials in Brazil have explored intranasal POH delivery as an alternative to circumvent the toxic limitations of oral administration. In these trials, patients with recurrent malignant gliomas were given comparatively small doses of POH via simple inhalation through the nose. Results from these studies showed, that this type of long-term, daily chemotherapy was well tolerated and effective. The precise mechanism of action is still undetermined, but it is known, that perillyl alcohol plays an important role in the process of hepatoma cell invasion and migration via decreasing the activity of Notch signaling pathway and increasing E-cadherin expression regulated by Snail. Another possible mechanism is included inhibition of Na/K-ATPase (NKA). The NKA α1 subunit is known to be superexpresses in glioblastoma cells (GBM) and POH acts in signaling cascades associated with NKA can control cell proliferation and/or cellular death.
Status:
Designated
Source:
FDA ORPHAN DRUG:453314
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Perilla alcohol is a naturally occurring monoterpene related to limonene. It is isolated from the essential oils of lavender, peppermint, spearmint, cherries, celery seeds, and several other plants. It has been used topically as a mosquito repellant and in toiletries and may be touted as a constituent of natural products such as tart cherry juice. Perillyl alcohol has demonstrated antiangiogenesis and anticancer effects in vitro. Purported mechanism of action is suppression of the synthesis of small G proteins, including RAS, thereby arresting tumor cells in the G1 phase of the cell cycle. Early clinical studies did not efficacy in prostate, ovarian or breast cancer, probably due to bad pharmacokinetic properties and toxicity after oral administration. More recent preliminary studies found intranasal delivery in patients with malignant gliomas to be well-tolerated and effective, with one study reporting tumor size regression, and another reporting increased overall survival and no side effects after long-term use.