Tecalcet (also known as KRN-568; NPS-R-568; R-568), is an oral calcium channel agonist potentially for the treatment of hyperparathyroidism. Calcimimetics, such as Tecalcet, are agonists and activate the calcium channel in a non-competitive fashion. Tecalcet does not compete directly with calcium that activates the receptor through binding in the extracellular domain of these receptors, but rather, calcimimetics such as Tecalcet, bind allosterically in the seven transmembranes to ‘sensitize’ the receptor to extracellular calcium. Tecalcet acts as an agonist of the calcium receptors of the parathyroid cells, causing a decrease in PTH release. Tecalcet also acts on the parafollicular cells (C-cells) of the thyroid gland, resulting in an increase in calcitonin release. These effects ultimately lead to a decrease in plasma calcium concentrations. Studies in rats have shown that oral administration of R-568 at doses ranging from 3 to 100 mg/kg caused a rapid (<30 minutes) decrease in plasma PTH concentrations and an increase in calcitonin concentrations, accompanied by a dose-dependent decrease in calcium concentrations. Tecalcet had been in phase II clinical trials by for the treatment of hyperparathyroidism, postmenopausal osteoporosis and rheumatic disorders in Japan and US. Development of Tecalcet has been discontinued.

Brefonalol also known as BDF 8186, a beta-adrenergic blocking agent with vasodilating properties. This drug was being developed for the treatment of hypertension, arrhythmias and angina pectoris. However, these studies were discontinued.

E7107 is a semisynthetic derivative of the natural product pladienolide B which was originally isolated from Streptomyces platensis. E7107 is the first compound a new class of anti-cancer agents targeting the spliceosome. Specifically E7107 interacts with the Splicing factor 3B subunit 1 (SF3b1) to block the normal splicing of oncogenes. Development of E7107 was suspended after Phase I clinical trials due to an unacceptable profile of adverse events.

Iodofiltic Acid I-123 is a single-photon branching free fatty acid radiopharmaceutical with potential application in single-photon emission computed tomography (SPECT). Assessment of fatty acid metabolism by radionuclide techniques has a potential role for the early detection of myocardial ischaemia and the assessment of the severity of ischaemic heart disease. The Iodofiltic Acid I-123 scan is preferable because it can provide suitable information for risk stratification just after an acute myocardial infarction (AMI) without requiring the patient to exercise; it can also detect previous ischaemic insult even after recovery of myocardial perfusion, the so- called "ischaemic memory".

Forminitrazole was studied as an antiprotozoal and antitrichomonal agent. Information about the current use of this compound is not available.

ISAGLIDOLE, an imidazoline derivative, is an alpha2-adrenoceptor antagonist. It stimulates insulin release in animal studies.

ISALSTEINE is a mucolytic agent.

ISOXAPROLOL is a potent beta-adrenoceptor antagonist with antihypertensive properties. It was effective in lowering blood pressure in acute trials on spontaneously hypertensive rats at a dosage of 15 mg/kg.

Bombesin (BN), a neuropeptide that originally was purified from the skin of the European frog (Bombina bombina). It has many biological effects including hormone release, stimulation of pancreatic enzyme secretion, gallbladder contraction and bronchoconstriction. Bombesin is a highly specific marker of neuroendocrine differentiation and thus a valuable tumor marker. It activates three different G-protein-coupled receptors known as BBR1, -2, and -3.