Posaconazole is a triazole antifungal drug that is used to treat invasive infections by Candida species and Aspergillus species in severely immunocompromised patients. It marketed in the United States, the European Union, and in other countries by Schering-Plough under the trade name Noxafil. Noxafil is used for prophylaxis of invasive Aspergillus and Candida infections in patients, 13 years of age and older, who are at high risk of developing these infections due to being severely immunocompromised as a result of procedures such as hematopoietic stem cell transplant (HSCT) recipients with graft-versus-host disease (GVHD), or due to hematologic malignancies with prolonged neutropenia from chemotherapy. Also for the treatment of oropharyngeal candidiasis, including oropharyngeal candidiasis refractory to itraconazole and/or fluconazole. Posaconazole blocks the synthesis of ergosterol, a key component of the fungal cell membrane, through the inhibition of cytochrome P-450 dependent enzyme lanosterol 14α-demethylase responsible for the conversion of lanosterol to ergosterol in the fungal cell membrane. This results in an accumulation of methylated sterol precursors and a depletion of ergosterol within the cell membrane thus weakening the structure and function of the fungal cell membrane. This may be responsible for the antifungal activity of posaconazole. It is absorbed within three to five hours and predominately eliminated through the liver, and has a half-life of about 35 hours. Oral administration of posaconazole taken with a high-fat meal exceeds 90% bioavailability and increases the concentration by four times compared to fasting state.

Corifungin refers to the sodium salt of amphotericin B. Although amphotericin B has become the primary drug of choice for treating primary amoebic meningoencephalitis, its use is associated with multiple side effects, including use-limiting renal toxicity. Initial reports for the in vivo efficacy of corifungin in a mouse model of primary amoebic meningoencephalitis showed activity superior to that of amphotericin B at equivalent dosing. Chemically, corifungin is the sodium salt of amphotericin B with excellent aqueous solubility. The increased solubility of corifungin is likely to account for the described increase in activity. Acea Biotech is developing corifungin for the treatment of fungal infections and amebic diseases. Acea has completed of host of animal studies on corifungin setting the stage to take the drug into the clinic. U.S. FDA has approved orphan drug status for corifungin for the treatment of primary amebic meningoencephalitis.

Aporeine (Roemerine) is an aporphine alkaloid that can be isolated from many plants such as Annona senegalensis, Turkish Papaver and Rollinialeptopetala. Aporeine has been reported to exhibit antibacterial activity. It has also been demonstrated to have certain antifungal activity. Aporeine showed selective inhibitory effect on Cox-2.

Radix Phytolaccae (the dried root of Phytolacca acinosa Roxb. or Phytolacca americana L.) is widely used in East Asian countries for the treatment of inflammation-related diseases. The active component of Radix Phtolaccae is Phytolcaccagenin a triterpenoid saponin. Phytolcaccagenin has anti-inflammatory activities that exceed those of Esculentoside A and its derivatives regarding suppression of LPS-induced inflammation, and has a lower toxicity profile with less hemolysis. Phytolaccagenin has promising antifungal activity against ATCC standard cultures of Candida albicans and Cryptococcus neoformans, and against clinical isolates of these fungi.

Arabinitol is the five-carbon sugar alcohol D-arabinitol (DA). It is a metabolite of the pathogenic Candida species, in vitro as well as in vivo, and can be determined by gas chromatography or enzymatic analysis. Endogenous DA and L-arabinitol (LA) are present in human body fluids. Serum DA and LA increase in renal dysfunction. In prospective clinical studies, elevated DA/LA or DA/creatine ratios in serum or urine have been found in immunocompromised, usually neutropenic, patients with invasive candidiasis. In addition, positive DA results have been obtained several days to weeks before positive blood cultures, and the normalization of DA levels has been correlated with therapeutic response in both humans and animals. Thus, arabinitol has been suggested a marker for invasive candidiasis. A non-invasive, non-culture-based method of determining urinary D-/L-arabinitol (D-/L-ARA) ratios was investigated as a tool for the diagnosis of invasive candidiasis in nosocomial paediatric infection cases in the clinical trial.

Benzoylmesaconine (BMA) is the main Aconitum alkaloid in Radix Aconiti Lateralis Preparata. Notably, the high levels of toxicity of Radix Aconiti are derived from diester aconitum alkaloids, including aconitine, mesaconitine and hypaconitine, which can be hydrolyzed to benzoylaconine, benzoylmesaconine and benzoylhypaconine, respectively. Benzoylmesaconine exhibits biological effects, including analgesic, antiviral and antifungal activities.

Helvolic acid is a mycotoxin with antibacterial activity that shows broad activity against Gram positive and negative bacteria. For example Helvolic acid showed potent inhibitory effects against Staphylococcus aureus and Pseudomonas aeruginosa with MIC (minimum inhibitory concentration) values of 5.8 and 4.6ug/mL, respectively. It is a steroidal triterpene that is an inhibitor of the protein biosynthesis through archeal EF-2 (elongation factor 2). Shows antioxidant effects. Helvolic acid also showed in vitro antitrypanosomal activity against Trypanosoma brucei brucei. It showed inhibitory activity against Candida albicans and Plasmodium falciparum.

(E)-2-decenoic acid is a stereoisomer of the corresponding medium-chain fatty acid in the trans configuration. This compound excreted by the caries bacterium Streptococcus mutants and inhibits the morphological transition from yeast to hyphae, an important virulence trait, in the opportunistic fungus Candida albicans. As a component of royal jelly it exhibits estrogenic effect by activation of estrogen receptor beta. Ethyl ester of trans-2-decenoic acid exerts neurotrophin-like neurotrophic activities in animal models of stress-induced anxiety-like, cerebral infarction and spinal cord injury.

Geraniol is a dietary monoterpene alcohol that is found in the essential oils of aromatic plants. To date, experimental evidence supports the therapeutic or preventive effects of geraniol on different types of cancer, such as breast, lung, colon, prostate, pancreatic, and hepatic cancer, and has revealed the mechanistic basis for its pharmacological actions. In addition, geraniol sensitizes tumor cells to commonly used chemotherapy agents. Geraniol controls a variety of signaling molecules and pathways that represent tumor hallmarks; these actions of geraniol constrain the ability of tumor cells to acquire adaptive resistance against anticancer drugs. It has been shown that geraniol inhibits HMG-CoA reductase in most types of tumor cells, which raises the possibility that the reduced prenylation of small G-proteins, such as Ras or RhoA, accounts for the antitumor effects of geraniol. In addition to its use in various commercial products, including cosmetics and fine fragrances, geraniol exerts a broad spectrum of pharmacological activities, such as anti-microbial, anti-inflammatory, anti-oxidant, anti-ulcer and neuroprotective activities. Geraniol is classified into the generally recognized-as-safe (GRAS) category by the Flavor and Extract Manufacturers Association (FEMA) and the Food and Drug Administration (FDA) of the United States.

Suloctidil is considered to be calcium antagonist. In addition to its vascular antispasmodic activity, suloctidil affects blood platelets and enhances brain energy metabolism. Suloctidil was being evaluated in many clinical trials for use in dementia and thrombotic disorders. Suloctidil induces hepatotoxicity.