Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Accession Number
Small Molecule

Icaridin, also known as Picaridin or hydroxy-ethyl isobutyl piperidine carboxylate, is a cyclic amine and a member of the piperidine chemical family. Piperidines are structural components of piperine, which is a plant extract from the genus _Piper _, or pepper. Icaridin has been commonly used as a topically-applied insect repellent in various countries but was officially licensed for use in the United States in 2001 and Canada in 2012 4. Icaridin was synthesized by Bayer in the 1980s based on molecular modeling 4. It is considered to be the first choice of repellent by the Public Health Agency of Canada’s Canadian Advisory Committee on Tropical Medicine and Travel for travelers six months to 12 years of age 1. Icaridin is reported to be less irritating than Diethyltoluamide, another common insect repellant, and products containing up to 20% of icaridin are considered safe for long-term use in adults 3.

  • Icaridin
  • Icaridina
  • Icaridinum
  • Picaridin
  • Pikaridin
  • Propidine
External IDs
EC 423-210-8 / KBR 3023
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
SG Plus Repellent Aroma MistLiquid2.1 g/30mLTopicalHankook Samgong Co.,ltd2017-06-27Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
SG Plus Repellent Aroma MistIcaridin (2.1 g/30mL)LiquidTopicalHankook Samgong Co.,ltd2017-06-27Not applicableUs
International/Other Brands
Bayrepel / Saltidin
CAS number
Average: 229.3159
Monoisotopic: 229.167793607
Chemical Formula
InChI Key
butan-2-yl 2-(2-hydroxyethyl)piperidine-1-carboxylate



Icaridin is indicated for use to repel insects, such as mosquitoes, biting flies, ticks, chiggers, and fleas, via topical use or over clothing 5.

Associated Conditions

Icaridin is a cyclic amine and piperidine compound that is expected to stimulate the sensory hairs on the antennae of insects 4.

Mechanism of action

The exact mechanism and target molecules of icaridin repelling insects are not fully understood; it is presumed that piperine interacts with the olfactory system consisting of odorant receptors (ORs) that need a common co-receptor (ORCO), and of ionotropic receptors (IR) 3, leading to the insect's inability to recognize its host's cues 4. It is also suggested that icaridin may bind to odorant binding protein 1 (AgamOBP1) at different binding sites 2. A study demonstrated that icaridin inhibited the odorant-induced responses of AaOR2 and AaOR8 expressed in Xenopus oocytes, leading to altered olfactory inputs by olfactory sensory neurons (OSN) 3.

AOdorant binding protein
Anopheles gambiae
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

Learn more
Additional Data Available

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

Learn more
Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more

In a dermal metabolism rat study, dermal application of 20 mg/kg of radio-labeled icaridin resulted in 61-66% of the dose absorbed through the skin 4. Following topical application of 20 mg/kg on rats, the peak plasma concentrations were measured to be 0.5 μg/mL in male rats and 0.8-1.6 μg/mL in female rats 4. In a study of human volunteers, less than 6% of the applied doses were absorbed after topical application of 14.7 or 15.0 mg of technical grade icaridin and covering the application site with a protective wrap for eight hours 4.

Volume of distribution

In a rat study, dermal application of icaridin at doses of either 20 mg/kg or 200 mg/kg resulted in plasma concentrations ranging from 0.5 μg/ml for males and 0.8-1.6 μg/ml for females in the 20 mg/kg test group, and 4.48 μg/ml in male rats and 1.70 μg/ml and female rats in the 200 mg/kg test group 4. Icaridin applied to the arms of human volunteers was not found in blood plasma 4.

Protein binding

There is no available information on the protein binding of icaridin.


There is limited data on the metabolism and resulting metabolites of the drug; however, it is estimated that icaridin undergoes phase I metabolic reactions involving 2-methylpropyl side chain or the piperidine ring being hydroxylated 4. It is also noted that the hydroxyethyl sidechain was oxidized to produce a carbonyl group. There was very little Phase 2 metabolism of the icaridin 4.

Route of elimination

Following topical administration on rats at doses of 20 mg/kg, urinary excretion was reported to be the primary route of elimination where 73-88% of the parent compound was recovered in the urine 4. At doses of 200 mg/kg, 33-40% of the administered dose was excreted in the urine or feces 4. No data were available on the composition of parent compound and metabolites in the urine of either animals or humans 4.

Half life

The first elimination half-lives of icaridin were determined in a study of five male and female rats treated with a single dose of 20 mg/kg icaridin dermally. The half-lives were 35.7 hours for male and 23.9 hours in female rats 6. In another study of rats treated daily for 2 weeks with 20 mg/kg of unlabeled icaridin, followed by exposure to a single dose of 20 mg/kg of the radiolabeled icaridin for 7 days, the 1st elimination half-lives were 10.9 and 9.1 hours for the males and females, respectively 6. The 2nd half-lives were 144 and 105 hours, respectively 6.


There is no available information on the clearance of icaridin.


Oral LD50 values in fasted and non-fasted male rats were 2236 mg/kg and 4743 mg/kg, respectively 4. Acute dermal LD50 values in rats were greater than 2000 mg/kg and 5000 mg/kg 4. The LC50 over a 4-hour exposure period exceeded 4364 mg/m^3 in male rats, and the NOEL was determined to be 2153 mg/m^3 4. While icaridin is considered to be practically non-toxic upon dermal and inhalation exposure 4, there have been cases of allergic contact dermatitis associated with pruritis and erythema upon dermal application 6.

In an animal study following application of icaridin to the skin of rats at doses of 50, 100, or 200 mg/kg/day each weekday for two years, there were no signs of potential carcinogenicity 4. The United States Environmental Protection Agency claims that icaridin is not likely to be carcinogenic to humans 6. In a two-generation reproductive study on rats, administering 50, 100, or 200 mg/kg icaridin to the rats' skin weekly beginning 10 weeks before mating and continuing through to weaning of the pups. Findings from the study concluded that chronic icaridin exposure to the skin at doses as high as 200 mg/kg did not result in reproductive toxicity 4.

Affected organisms
  • Scabies (Sarcoptes scabei) and other insects
Not Available
Pharmacogenomic Effects/ADRs
Not Available


Drug Interactions
OxybenzoneOxybenzone can cause a decrease in the absorption of Icaridin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Evidence Level

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
Not Available


General References
  1. Onyett H: Preventing mosquito and tick bites: A Canadian update. Paediatr Child Health. 2014 Jun;19(6):326-32. [PubMed:25332663]
  2. Drakou CE, Tsitsanou KE, Potamitis C, Fessas D, Zervou M, Zographos SE: The crystal structure of the AgamOBP1*Icaridin complex reveals alternative binding modes and stereo-selective repellent recognition. Cell Mol Life Sci. 2017 Jan;74(2):319-338. doi: 10.1007/s00018-016-2335-6. Epub 2016 Aug 17. [PubMed:27535661]
  3. Van Roey K, Sokny M, Denis L, Van den Broeck N, Heng S, Siv S, Sluydts V, Sochantha T, Coosemans M, Durnez L: Field evaluation of picaridin repellents reveals differences in repellent sensitivity between Southeast Asian vectors of malaria and arboviruses. PLoS Negl Trop Dis. 2014 Dec 18;8(12):e3326. doi: 10.1371/journal.pntd.0003326. eCollection 2014 Dec. [PubMed:25522134]
  4. Gervais, J. A.; Wegner, P.; Luukinen, B.; Buhl, K.; Stone, D. 2009. Picaridin Technical Fact Sheet; National Pesticide Information Center, Oregon State University Extension Services. [Link]
  5. DailyMed - SG PLUS REPELLENT AROMA MIST- icaridin liquid [Link]
  6. PICARIDIN - National Library of Medicine HSDB Database - Toxnet - NIH [Link]
  7. Health Canada Icaridin Evaluation [File]
External Links
Download (22.5 KB)

Clinical Trials

Clinical Trials
Not Available


Not Available
Not Available
Dosage forms
LiquidTopical2.1 g/30mL
Not Available
Not Available


Experimental Properties
melting point (°C)< -170O'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Cambridge, UK: Royal Society of Chemistry, 2013., p. 1373
boiling point (°C)208 at 1013 hPaO'Neil, M.J. (ed.). The Merck Index - An Encyclopedia of Chemicals, Drugs, and Biologicals. Cambridge, UK: Royal Society of Chemistry, 2013., p. 1373
water solubilityInsolublePicaridin Technical Fact Sheet; National Pesticide Information Center, Oregon State University Extension Services.
Predicted Properties
Water Solubility25.1 mg/mLALOGPS
pKa (Strongest Acidic)15.92ChemAxon
pKa (Strongest Basic)-2.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area49.77 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity62.54 m3·mol-1ChemAxon
Polarizability26.24 Å3ChemAxon
Number of Rings1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available


Mass Spec (NIST)
Not Available
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available


Not classified


Anopheles gambiae
Pharmacological action
General Function
Not Available
Specific Function
Odorant binding
Gene Name
Uniprot ID
Uniprot Name
Odorant binding protein
Molecular Weight
16538.985 Da
  1. Drakou CE, Tsitsanou KE, Potamitis C, Fessas D, Zervou M, Zographos SE: The crystal structure of the AgamOBP1*Icaridin complex reveals alternative binding modes and stereo-selective repellent recognition. Cell Mol Life Sci. 2017 Jan;74(2):319-338. doi: 10.1007/s00018-016-2335-6. Epub 2016 Aug 17. [PubMed:27535661]

Drug created on June 16, 2018 17:17 / Updated on May 01, 2019 11:56