General
Preferred name
CANTHARIDIN
Synonyms
NSC-61805 ()
Cantharidinum ()
Cantharidine ()
Ycanth ()
Cantaridina ()
Cantharides camphor ()
P&D ID
PD011789
CAS
56-25-7
Tags
available
drug
natural product
Approved by
FDA
First approval
2023
Drug indication
Molluscum contagiosum infection
Rheumatoid arthritis
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
INDICATION The only therapeutic use for which cantharidin is currently primarily indicated for is as an active ingredient in topical agents for treating common warts (verruca vulgaris), periungual warts, plantar warts, and molluscum contagiosum [A32891, A32892, F32]. ; ; At the same time, such topical cantharidin applications have also been used for a number of off-label indications like callus removal, cutaneous leishmaniasis, herpes zoster, and acquired perforating dermatosis [A32892]. Furthermore, since most topical cantharidin applications are most commonly available in a 0.7% formulation or a more potent 1% mixture, the 0.7% formulation is most commonly indicated for the treatment of common warts, periungual warts, and molluscum contagiosum while the more potent 1% mixture is typically limited only for use by healthcare professionals in a clinical setting for treating plantar warts and other more specialized off-label conditions [A32891, A32892, F32].; ; Moreover, there have also been studies into whether or not cantharidin could be effective at being used as an inflammatory model or in cancer treatment - either of which has yet to formally elucidate any results [A32892].
ROE It has been observed that absorbed cantharidin is excreted by the kidney [L2648].; ; Little pharmacodynamic and pharmacokinetic data regarding cantharidin in the human body currently exists; recruitment for First-Time-In-Human clinical trials regarding such information have been ongoing in 2018 [L2647]. There are however some studies regarding such data in animal models like beagle dogs [A32901].
ABSORPTION Cantharidin is absorbed from the gastrointestinal tract, and, to a limited extent from the skin as well [L2648].; ; Little pharmacodynamic and pharmacokinetic data regarding cantharidin in the human body currently exists; recruitment for First-Time-In-Human clinical trials regarding such information have been ongoing in 2018 [L2647]. There are however some studies regarding such data in animal models like beagle dogs [A32901].
DESCRIPTION Cantharidin is a terpenoid substance that is secreted by insects such as male blister beetles. It is also synthetically manufactured. Cantharidin causes skin blisters in humans, and can be highly toxic if ingested in sufficient quantity. (GtoPdb)
MOA Cantharidin is specifically absorbed by lipids in the membrane of epidermal keratinocytes, where it activates the release of neutral serine proteases [A32891, A32892]. These enzymes subsequently break the peptide bonds in surrounding proteins, leading to the progressive degeneration of desmosomal dense plaques, which are important cellular structures that participate in cell-to-cell adhesion [A32891, A32892]. Such degeneration results in the detachment of the tonofilaments that hold cells together. This process as a whole leads to the selective acantholysis (loss of cellular connections) and blistering of the skin when the cantharidin topical application is applied upon specific topical developments like warts [A32891, A32892]. A blister(s) at the application site develop within 24 to 48 hours of application and typically resolve within 4 to 7 days [A32891, A32892]. Factors that can modify this proposed time frame include the volume or concentration of cantharidin used, physical contact time of the applied compound (usually between 4 to 24 hours), the presence of any occlusive dressings, or even patient sensitivity to cantharidin [A32891, A32892]. The blistered lesions ultimately heal without scarring [A32891, A32892].; ; Finally, there are some studies that suggest cantharidin's chemical profile as a potent and selective inhibitor of protein phosphatase 2A confers upon it an oxidative stress-independent growth inhibition of pancreatic cancer cells through cancer cell-cycle arrest and apoptosis [A32900]. ; ; Nevertheless, the fact that little data regarding the pharmacodynamics and pharmacokinetics of cantharidin in the human body exists [L2647] and certain toxic effects of cantharidin that have been observed following oral ingestion in humans like ulceration of the gastrointestinal and genitourinary tracts, along with electrolyte and renal function disturbance [A32891] are strong reasons as to why the compound currently lacks FDA approval is used fairly limitedly for formal therapeutic indications.
PRICE 29
DESCRIPTION Cantharidin, a natural toxin found in beetles in the families Meloidae and Oedemeridae, has been reported to be toxic to some pests, including the diamondback moth.
DESCRIPTION Cyclooxygenase-1 (COX-1) inhibitor (Tocris Bioactive Compound Library)
DESCRIPTION Protein phosphatase 1 and 2A inhibitor (Tocriscreen Total)
Cell lines
20
Organisms
2
Compound Sets
18
Cayman Chemical Bioactives
14589
ChEMBL Approved Drugs
CHEMBL48449
ChEMBL Drugs
CHEMBL48449
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB12328
DrugBank Approved Drugs
DB12328
DrugCentral
5743
DrugCentral Approved Drugs
5743
DrugMAP
DMBP5N3
DrugMAP Approved Drugs
DMBP5N3
EU-OPENSCREEN Bioactive Compound Library
EOS100663
Guide to Pharmacology
13081
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL48449
NIH Mechanistic Set
Reference compounds for characterizing cellular injury in high-content cellular morphology assays
Tocris Bioactive Compound Library
1548
Tocriscreen Total
External IDs
33
Properties
(calculated by RDKit )
Molecular Weight
196.07
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
0
Rotatable Bonds
0
Ring Count
3
Aromatic Ring Count
0
cLogP
0.64
TPSA
52.6
Fraction CSP3
0.8
Chiral centers
4.0
Largest ring
5.0
QED
0.42
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Primary Target
Protein Ser/Thr Phosphatases
MOA
Inhibitor
protein phosphatase inhibitor
Indication
blisters
Cellular injury category
Miscellaneous
Source data