AMPHOTERICIN B CHOLESTERYL SULFATE COMPLEX (AMPHOTEC) is an antifungal medicine. AMPHOTEC® is a sterile, pyrogen-free, lyophilized powder for reconstitution and intravenous (IV) administration. AMPHOTEC consists of a 1:1 (molar ratio) complex of amphotericin B and cholesteryl sulfate. AMPHOTEC is indicated for the treatment of invasive aspergillosis in patients where renal impairment or unacceptable toxicity precludes the use of amphotericin B deoxycholate in effective doses, and in patients with invasive aspergillosis where prior amphotericin B deoxycholate therapy has failed. The active ingredient of AMPHOTEC, amphotericin B, is a polyene antibiotic that acts by binding to sterols (primarily ergosterol) in cell membranes of sensitive fungi, with subsequent leakage of intracellular contents and cell death due to changes in membrane permeability. Amphotericin B also binds to the sterols (primarily cholesterol) in mammalian cell membranes, which is believed to account for its toxicity in animals and humans. AMPHOTEC is active against Aspergillus spp (A. fumigatus, A. flavus), Candida spp (C. albicans, C. krusei, C. parapsilosis, C. tropicalis), Cryptococcus neoformans, and Blastomyces dermatitidis. Active against most fungi with the notable exceptions of Candida lusitaniae, Trichosporon beigelii, Aspergillus terreus (some isolates), Pseudallescheria boydii, Malassezia furfur and Fusarium spp. The lipid formulations are designed to reduce binding of amphotericin to mammalian cell membranes, therefore reducing toxicities.

GSK 1059615, a pyridinylquinoline derivative, is a novel PI3K kinase and mTOR dual inhibitor. GSK1059615 was in phase I clinical trial in patients with solid tumors or lymphoma, but this study was terminated prematurely due to lack of sufficient exposure following single- and repeat dosing. In addition, recently was shown, that GSK 1059615 in xenograft mice models possessed anti-head and neck squamous cell carcinoma (HNSCC) cell activity.

AN-2718 is a member of a new class of antifungals, benzoxaboroles, which inhibit fungal growth by blocking protein synthesis. AN-2718 is being developed for the topical treatment of tinea pedis including the hard to treat mocassin-type, which at present is only treatable with oral antifungals. AN-2718 inhibits an essential protein synthesis enzyme, leucyl-transfer RNA synthetase, or LeuRS. AN-2718 Inhibits LeuRS by the OBORT mechanism of trapping tRNALEU in the editing site of LeuRS. AN-2718 has good MIC90 activity against the dermatophytes, T. rubrum and T. mentagrophytes, which supports its use as a topical agent to treat tinea pedis. AN-2718 has been used in trials studying Tinea Pedis, but its development has been discontinued.

MK-2206 is an oral selective allosteric inhibitor of Akt that targets all three isoforms of human Akt (Akt-1, Akt-2 and Akt-3). In a phase I study of solid tumors, MK-2206 demonstrated evidence of target modulation and anti-proliferative activity as a single agent and in combination with other agents. Current ongoing trials of MK-2206 include monotherapy and combination therapy in breast cancer, colorectal cancer, haematological malignancies, non-small cell lung cancer and other. Detected treatment-related adverse event are: rash, fatigue, hyperglycemia.

Calcium Cation Ca-45 is a calcium radioactive isotope which used for evaluation of calcium absorption and intracellular concentration in scientific research. There are several calcium radionuclides available, including 41Ca, 45Ca, and 47Ca. For practical reasons, 45Ca is the most commonly used calcium radionuclide for biological investigations.

Calcium Cation Ca-47 is a rare calcium radioactive isotope which used in orthopaedics for bone formation evaluation. Calcium-47 has a half-life of about five days, which is long enough for numerous biological investigations and short enough to ensure that the person subjected to the investigation is not under prolonged irradiation. It emits gamma rays in addition to beta rays, and since the gamma rays are capable of penetrating many centimeters of tissue, determination of calcium-47 in the body is possible by external measurements. Unfortunately, calcium-47 is difficult to produce and did not use in routine medical practice

Veledimex is an oral activator ligand for a proprietary gene therapy promoter system, and a moderate inhibitor of and substrate for CYP3A4/5. Veledimex controls the expression of the target gene. The amount of gene product produced by the system and the duration of the effect is dependent on veledimex dose level and duration of dosing. Nonclinical studies demonstrated that intratumoral administration of Ad-RTS-IL12 along with oral administration of veledimex elicited dose-dependent anti-tumor effects in murine melanoma, breast cancer and glioma models which correlated with increased plasma exposure of veledimex. The FDA granted Fast Track designation for Ad-RTS-hIL-12 plus veledimex for the treatment of recurrent or progressive glioblastoma multiforme in adults. Ad-RTS-hIL-12 is an inducible adenoviral vector encoding human pro-inflammatory cytokine interleukin-12 (IL-12), which is under the transcriptional control of the RheoSwitch Therapeutic System. Veledixmex is an oral activator ligand. Data previously presented suggest that Ad-RTS-hIL-12 with 20 mg veledimex improves the median overall survival from 6 to 9 months seen with available therapies to 12.7 months, with further improvement in median overall survival to 17.8 months in a subset of subjects with reduced cumulative steroid exposure during the active dosing period of veledimex. Veledimex has been used in trials studying the treatment of glioblastoma multiforme, metastatic breast cancer, and anaplastic oligoastrocytoma.