Pittsburgh compound B (PiB) is a radioactive analog of thioflavin T, which can be used in positron emission tomography scans to image beta-amyloid plaques in the brains of patients with Alzheimer’s disease. 11C-PIB specifically binds to Aβ40 and Aβ42 fibrils and insoluble plaques containing the aforementioned Aß peptides with no detectable binding to soluble Aβ forms or neurofibrillary tangles under PET study conditions. Furthermore, this radiotracer does not bind to neurofibrillary tangles (NFTs) in the neuronal regions of the brain during postmortem autopsies. A typical injected dose ranges from 250-450 MBq and the imaging time normally varies between 40 and 90 minutes. The quantification of 11C-PIB has demonstrated to elicit a profound difference in neuronal cortical binding between individuals recognized with Alzheimer's disease and age-matched cognitively normal controls.

Ridaforolimus (Deforolimus, MK-8669) is an investigational oral mTOR inhibitor in development for the treatment of metastatic soft-tissue or bone sarcomas. Ridaforolimus is being co-developed by Merck and ARIAD Pharmaceuticals. Ridaforolimus (Deforolimus, MK-8669) is a selective mTOR inhibitor with IC50 of 0.2 nM in HT-1080 cell line; while not classified as a prodrug, mTOR inhibition and FKBP12 binding is similar to rapamycin. mTOR is a protein kinase that controls cell growth by regulating many cellular processes, including protein synthesis and autophagy. Compared with other mTOR inhibitors, ridaforolimus is not a prodrug and has shown in vivo stability. Both intravenous and oral formulations of the compound are being tested in clinical trials for the treatment of various solid tumors and hematologic malignancies. The initial indication is soft-tissue and bone sarcomas. Ridaforolimus was indicated to treat patients with metastatic soft tissue sarcoma or bone sarcoma whose disease has not progressed after at least 4 cycles of chemotherapy. In June 2012, Merck & Co., Inc. announced the receipt of a Complete Response Letter from the U.S. Food and Drug Administration (FDA), advising the company that the New Drug Application (NDA) for ridaforolimus had not been approved. Currently Ridaforolimus is in phase III clinical trials for the treatment of Coronary artery restenosis.

Endralazine (6-benzoyl-3-hydrazino-5,6,7,8-tetrahydropyrido-(4,3-c)-pyridazine mesylate) is a peripheral vasodilator drug, which acts by direct relaxation of the smooth muscle fibres of the peripheral arterial vessels. Endralazine has been used as an antihypertensive agent.

Hepronicate is a nicotinic acid derivative, developed and used in Japan under the name Megrin for the treatment of peripheral circulatory disorders. The therapeutic effect of the drug is explained by its vasodilation properties.

Glafenine is a non-steroidal anti-inflammatory drug (NSAID). Glafenine was withdrawn due to the risk of anaphylaxis and acute kidney failure.

Glyparamide is the chlorophenyl-containing oral hypoglycemic sulfonamide. Glyparamide rarely causes hepatic injury.

Aranidipine (INN, trade name Sapresta) is a calcium channel blocker. Calcium channel antagonists have become popular medications for the management of hypertension. These agents belong to the diphenylalkylamine, benzothiazepine, dihydropyridine, or tetralol chemical classes. Although the medications share a common pharmacological mechanism in reducing peripheral vascular resistance, clinical differences between the sub-classes can be linked to structural profiles. This heterogeneity is manifested by differences in vascular selectivity, effects on cardiac conduction and adverse events. The lack of differentiation between calcium channel antagonists in clinical trials has contributed to uncertainty associated with their impact on morbidity and mortality. Administartion of aranidipine once daily had a high potent antihypertensive effect and clinical utility in all the clinical trials conducted in Japan. Aranidipine is now under registration.

Pralmorelin [GPA 748, GHRP 2, growth hormone-releasing peptide 2, KP-102 D, KP 102 LN] is an orally active, synthetic growth hormone-releasing peptide from a series of compounds that were developed by Polygen in Germany and Tulane University in the US. The use of pralmorelin as a diagnostic agent for GH deficiency is based on its ability to markedly increase plasma levels of GH in healthy subjects irrespectively of gender, obesity or age. However, in patients with GH deficiency, the effect of pralmorelin on GH levels is significantly lower compared with healthy controls. Pralmorelin is marketed under the brand name GHRP in Japan. It is used as a diagnostic agent in a single-dose formulation for the assessment of growth hormone deficiency (GHD). Pralmorelin (GHRP-2) acts to endogenously increase growth hormone release from the pituitary. With the increase of serum growth hormone, downstream effects occur. A notable hormone that is commonly used as a surrogate for growth hormone therapy, insulin like growth factor 1 (IGF-1), is known to increase with the infusion of GHRP-2. Administration of GHRP-2 results in amplification of the naturally occurring growth hormone secretion peaks, regulated by the hypothalamus and pituitary. After the release of growth hormone, a cascade of signaling events occurs in many body tissues, continuous exposure to growth hormone elicits long-term physiological changes. Of particular interest, especially in the case of the use of GHRP-2 as an alternative growth hormone therapy, hepatic production of IGF-1 occurs as result of endogenously released growth hormone from GHRP-2. GHRP-2 acts on the growth hormone secretagogue receptor (GHSR1a) in pituitary and hypothalamic tissues. The growth hormone secretagogue receptor (GHSR) is the natural receptor for the endogenous hormone Ghrelin, a stress hormone produced mainly by the lining of the stomach. This receptor among many other functions, controls and growth hormone release.

Acronine is an acridone alkaloid isolated from the bark of Acronychia bauri Schott, scrub ash indigenous to Australia. It possesses broad-spectrum activity against experimental neoplasms. Acronine has been studied in the treatment of multiple myeloma. Acronine analogues also possess cytotoxic and antitumor activity.

Pirisudanol is the succinic acid ester of pyridoxine (a form of vitamin B6) and of deanol that has been used in Europe in the treatment of mild cognitive impairment as well as fatigue and depression.