topical

Chloroxine (Capitrol) is a synthetic quinoline derivative with antibacterial activity. Although the mechanism of action is not fully understood, topical administration of chloroxine diminishes mitotic activity in the epidermis, thereby reducing excessive scaling associated with dandruff or seborrheic dermatitis of the scalp, including psoriasis and eczema.

Picaridin (Lcaridin) is a topical insect repellent.

Patchouli alcohol (Patchoulol) is a sesquiterpene alcohol found in patchouli oil. It has antibacterial, antifungal, and antiviral actions. Patchouli alcohol also suppresses inflammation induced by lipopolysaccharide in vivo. Topical application of patchouli alcohol accelerates recovery from ultraviolet irradiation-induced skin damage through antioxidant and anti-inflammatory effects.

Methyl nicotinate (methyl pyridine-3-carboxylate) is the methyl ester of that is used as an active ingredient as a rubefacient in over-the-counter topical preparations indicated for muscle and joint pain. The action of methyl nicotinate as a rubefacient is thought to involve peripheral vasodilation.

Chlorhexidine diacetate (Bactigras) is a disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque.

4-Isopropylcatechol is a potent depigmenting agent and is of use in the topical therapy of selected patients with hypermelanosis.

Efletirizine (UCB-28754) is a histamine receptor antagonist with inhibitory effects on the enzyme 5-lipoxygenase (5-LO), and is useful in the topical treatment of allergic diseases.

Ticolubant is orally active leukotriene B4 antagonist with high affinity for the human neutrophil LTB4 receptor (Ki = 0.78 nM), blocks LTB4-induced Ca2+ migration with an IC50 of 6.6 ± 1.5 nM, and shows topical anti-inflammatory activity in a mouse model of skin inflammation.

Safotibant (LF-22-0542) is a bradykinin B1 receptor antagonist with anti-inflammatory and analgesic activity for the topical treatment of diabetic macular edema.

Tanimilast (CHF-6001) is a novel, potent and selective phosphodiesterase 4 inhibitor with an IC 50 value of 0.026 ± 0.006 nM.Tanimilast has potent anti-inflammatory activity and is indicated for topical use in the lungs.Tanimilast was used in the study of obstructive lung disease.

Amantanium bromide (Amantanil bromidum) is a quaternary ammonium antibacterial/antifugal agent useful as a surgical antiseptic and for the topical therapy of mucous and cutaneous infections.

Algestone acetophenide (Neolutin) is progesterone that used in estrus synchronization and has been evaluated as an injectable contraceptive in combination with estradiol enanthate. It is also used therapeutically as a topical anti-inflammatory and is applied topically in the therapy of ACNE.

Diquafosol Tetrasodium is a P2Y2 receptor agonist that stimulates the secretion of mucins from ocular tissues Diquafosol tetrasodium (INS365) improves tear film stability and visual function, as a topical treatment of dry eye disease.

Chlorhexidine (Rotersept) is a biguanide compound used as an antiseptic agent with topical antibacterial activity. Chlorhexidine is positively charged and reacts with the negatively charged microbial cell surface, thereby destroying the integrity of the cell membrane. Subsequently, chlorhexidine penetrates into the cell and causes leakage of intracellular components leading to cell death. Since gram-positive bacteria are more negatively charged, they are more sensitive to this agent.

Nystatin (Fungicidin) is a topical and oral antifungal agent with activity against many species of yeast and candida albicans, which is used largely to treat skin and oropharyngeal candidiasis.

Resiquimod (R848) is an imidazoquinoline amine and Toll-like receptor (TLR) agonist with potential immune response modifying activity. Resiquimod exerts its effect through the TLR signaling pathway by binding to and activating TLR7 and 8 mainly on dendritic cells, macrophages, and B-lymphocytes. This induces the nuclear translocation of the transcription activator NF-kB as well as activation of other transcription factors. This may lead to an increase in mRNA levels and subsequent production of cytokines, especially interferon-alpha (INF-a) and other cytokines, thereby enhancing T-helper 1 (Th1) immune responses. In addition, topical application of resiquimod appears to activate Langerhans' cells, leading to an enhanced activation of T-lymphocytes.

Tazarotene (Zorac) is a synthetic, topical retinoid. Tazarotene induces the expression of tazarotene-induced gene 3 (TIG3), a tumor suppressor gene. In psoriasis, tazarotene normalizes abnormal keratinocyte differentiation and reduces their hyperproliferation.

Medrysone (6α-Methyl-11β-hydroxyprogesterone) is a topical, synthetic glucocorticoid with metabolic, anti-inflammatory and anti-allergic properties. Medrysone exerts its effect by interacting with specific intracellular glucocorticoid receptors and subsequently binds to DNA to modify gene expression. This results in an induction of the synthesis of certain anti-inflammatory proteins while inhibiting the synthesis of certain inflammatory mediators. Consequently, an overall reduction in chronic inflammation and autoimmune reactions is accomplished.

Nitrofurazone (Furacilin) is a topical anti-infective agent effective against gram-negative and gram-positive bacteria. It is used for superficial WOUNDS AND INJURIES and skin infections. Nitrofurazone(NFZ) has also been administered orally in the treatment of TRYPANOSOMIASIS.

Chlorhexidine dihydrochloride (NSC-185) is a disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque.

Fusidic acid sodium salt (SQ-16360) is a sodium salt form of fusidic acid, a bacteriostatic antibiotic derived from the fungus Fusidium coccineum and used as a topical medication to treat skin infections.

Oxethazaine (Oxetacaine), a topical anesthetic, is used to prevent acid-induced esophageal pain.

Tapinarof (Benvitimod) is targeted as a topical cream treatment for psoriasis, a chronic autoimmune skin disease.

Econazole ((±)-Econazol) is an imidazole derivative that is commonly used as a topical antifungal agent.

Piketoprofen (Calmatel) is a topical nonsteroidal anti-inflammatory agent.

(Rac)-MGV354 (MGV354) is the racemate of MGV354. MGV354 is a soluble activator of guanylate cyclase (sGC)(EC50s of <0.5 nM, and 5 nM in CHO and GTM-3 E cells, respectively).

Mafenide acetate, a sulfonamide, inhibits the enzyme carbonic anhydrase and is used as a topical anti-infective drug, especially in burn therapy.

PGF2α isopropyl ester is an ester prodrug of PGF2α with enhanced lipid solubility. Due to better membrane penetration, PGF2α isopropyl ester is more suitable than PGF2α or PGF2α tromethamine salt for topical application in studies on intraocular pressure. The ester functionality is readily hydrolyzed in vivo to release the active compound PGF2α. When administered topically to the eyes of cynomolgus monkeys, a 5 μg dose reduces intraocular pressure by 68% after the fourth day of treatment.

Proflavine dihydrochloride is a topical antiseptic.

ABT-281 is an ascomycin analog and a macrolactam T cell inhibitors with potent topical activity and reduced systemic exposure.

Halometasone is a synthetic corticosteroid.1,2Formulations containing halometasone have been used in the treatment of psoriasis vulgaris and eczematous dermatoses. 1.de la Brassine, M., Kint, A., Lachapelle, J.M., et al.Halomethasone (C 48.401-Ba) for the topical treatment of common dermatosesJ. Int. Med. Res.12(5)307-309(1984) 2.Zhu, J.-W., Wu, X.-J., Lu, Z.-F., et al.Role of VEGF receptors in normal and psoriatic human keratinocytes: Evidence from irradiation with different UV sourcesPLoS One8(1)e55463(2013)

BAY 1003803 is a glucocorticoid receptor agonist for the topical treatment of psoriasis or severe atopic dermatitis.

RS 85095 is a thiol ester corticosteroid that is topical.

Patulitrin has antioxidant, anti-inflammatory, and larvicidal activities, oral and topical administration of patuletin and patulitrin inhibited acute inflammation in mice.

Chlorindanol (Lanesta) is a new antiseptic agent. It is nonallergenic and appears to be suitable for use as a topical antiseptic or sanitizer.

Diphenylcyclopropenone (DPCP) is a topical drug used to treat alopecia areata, alopecia totalis, and refractory warts. Diphencyprone acts as a local stimulator that triggers an immune response against the action of autoreactive cells.

Nystatin A3 (Fungicidin) , which belongs to the polyene group of antimycotics, is frequently used as a topical agent in the treatment of oro-pharyngeal candidosis.

Betamethasone-17-butyrate-21-propionate is a topical corticosteroid and may be used in the treatment of inflammatory skin diseases.

Pseudomonic acid D is a topical antibiotic agent used against superficial skin infections such as impetigo or folliculitis.

Proparacaine Hydrochloride is the hydrochloride salt form of proparacaine, a benzoic acid derivative with local anesthetic property. Proparacaine hydrochloride (Proparacaine HCl) stabilizes the neuronal membrane by binding to and inhibiting voltage-gated sodium channels, thereby inhibiting sodium ion influx required for the initiation and conduction of impulses within the neuronal cell, and resulting in a loss of sensation.

LEO 134310, a selective, non-steroidal glucocorticoid receptor (GR) agonist, is optimized for topical treatment. Demonstrating high affinity (EC50 of 14 nM) in GR binding assays, it is suitable for treating skin diseases.

Sezolamide hydrochloride is a potent topical carbonic anhydrase inhibitor.

Flucloronide is a corticosteroid for topical use on the skin. It has anti-inflammatory properties.

Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bithionol drug products were withdrawn on October 24, 1967.

Rhinocaine is an antiarrythmic and a topical anesthetic.

Omiganan-FITC TFA, a compound integrating the bactericidal and fungicidal cationic peptide Omiganan with a fluorescein isothiocyanate (FITC), is under development as a topical gel aimed at preventing catheter-associated infections [1].

Sumarotene, a third-generation retinoid, is used as a topical dermatologic agent for the repair of antikeratinization, photodamage, and antiproliferation.

L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively[1][2]. L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunction[2].Intrathecal injection of 30 μg of L-AP4 does not significantly alter the paw withdrawal latency in these normal rats[2].Topical application of 5 to 50 μM L-AP4 to the spinal cord significantly inhibited the evoked response of neurons to touch, pressure, pinch, and von Frey filaments in a concentration-dependent fashion[2]. Animal Model: Rats.[2] [1]. Selvam C, et al. Increased Potency and Selectivity for Group III Metabotropic Glutamate Receptor Agonists Binding at Dual sites. J Med Chem. 2018 Mar 8;61(5):1969-1989. [2]. Chen SR, et al. Distinct roles of group III metabotropic glutamate receptors in control of nociception and dorsal horn neurons in normal and nerve-injured Rats. J Pharmacol Exp Ther. 2005 Jan;312(1):120-6.

GAT229 is a positive allosteric modulator of cannabinoid receptor 1 (CB1) and the S-(-) enantiomer of the CB1 modulator GAT211. It does not activate the receptor on its own but enhances the binding and activity of CB agonists. GAT229 (1 μM) enhances the binding of the CB1 full agonist CP 55,940 to CHO cells expressing human recombinant CB1 (hCB1), as well as the activity of 2-arachidonoyl glycerol , arachidonoyl ethanolamide , and CP 55,940 in arrestin2 recruitment assays and increases ERK1/2 and PLCβ3 phosphorylation in HEK293 cells expressing hCB1. GAT229 (1 μM) enhances depolarization-induced suppression of excitation but does not inhibit excitatory postsynaptic currents (EPSCs) in murine autaptic hippocampal neurons. GAT229 (0.2%, topical) reduces intraocular pressure by 5.8 and 7.7 mm Hg after 6 and 12 hours, respectively, in a transgenic mouse model of ocular hypertension using nose, ear, eye mutation (nee) mice.

Flutrimazole is a dual-action imidazole antifungal compound, exhibiting both anti-inflammatory and antifungal properties. Notably, flutrimazole demonstrates limited transdermal penetration, making it particularly advantageous for topical applications in the treatment of fungal infections, especially those accompanied by inflammation.