Tiplasinin (PAI-039) is an orally efficacious and selective plasminogen activator inhibitor-1 (PAI-1) inhibitor. Tiplasinin bound specifically to the active conformation of PAI-1 and exhibited reversible inactivation of PAI-1 in vitro. Tiplaxtinin exhibited in vivo oral efficacy in two different models of acute arterial thrombosis. The remarkable preclinical safety and metabolic stability profiles of tiplaxtinin led to advancing the compound to Phase-I clinical trial for Thrombosis, which was later discontinued.

LAMIFIBAN is a potent and selective nonpeptide glycoprotein IIb/IIIa antagonist. It inhibits platelet aggregation and thrombus formation by preventing the binding of fibrinogen to platelets. It was in clinical development as an injectable antithrombotic agent for treating and preventing acute coronary syndromes but showed no significant effects on clinical outcomes.

Naroparcil [LF 90055], the lead compound in a series of orally-active antithrombotics, is an analogue of LF 1351, a compound shown to have antithrombotic action. Antithrombotic activity of naroparcil is dependent on modification in the plasma GAG profile which inactivates thrombin via heparin cofactor II (HCII).

ISBOGREL is a specific thromboxane A2 synthetase inhibitor. Its clinical development was discontinued, although it was a suitable candidate for clinical trials in cardiovascular diseases in which imbalance between thromboxane and prostacyclin may be involved in the pathogenesis.

Odiparcil is a novel, orally active beta-d-thioxyloside analog with antithrombotic activity associated with a reduced risk of adverse bleeding events. Its unique mechanism of action is postulated by means of an elevation in circulating endogenous chondroitin sulfate-related glycosaminoglycans (GAGs) levels. Odiparcil has demonstrated good tolerability, safety and efficacy in phase I and phase IIa studies, in approximately 700 healthy volunteers and 1100 patients. The drug has been investigated in several preclinical models and its potential has been proven in MPS. It may be therefore anticipated that Odiparcil could prove beneficial to MPS patients (MPS I, II and VI) as a substrate reduction therapy as a stand-alone treatment on in adjunction to current treatments. U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation to odiparcil (formerly known as IVA336) for the treatment of mucopolysaccharidosis VI (MPS VI), also known as Maroteaux-Lamy syndrome.

Sulocarbilate (also known as W-1548-1) is a sulfanilamide derivative and carbonic anhydrase inhibitor with diuretic activity. In preclinical models, Sulocarbilate shows similar efficacy and superior safety profile compared to other agents of this type. Clinically, Sulocarbilate shows the maximum effect as a natriuretic agent in an oral daily dose of 2 g.

Sulosemide is a sulfamoylorthanilic acid derivative patented by German chemicals then life-sciences company Hoechst A.-G. as salidiuretic agent.

Gallium maltolate is an oral agent in development for the potential treatment of chronic bacterial infections, bone disease and cancer. The bioavailable form, composed of a trivalent gallium cation (Ga3+) competes with and replaces Fe3+ in many vital Fe 3+-mediated biological reactions, but cannot mimic Fe3+ functions. High amounts of iron are needed for DNA synthesis in cancer, and the incorporation of Ga3+ inactivates the Fe3+-dependent enzyme ribonucleotide reductase (RR), an enzyme essential for DNA synthesis, leading to an inhibition of DNA synthesis and induction of cell death in rapidly proliferating cells. Gallium similarly reduces bacterial cell growth. Ga3+ is also able to suppress inflammation through the down-regulation of pro-inflammatory cells and the inhibition of pro-inflammatory cytokine secretion. Other effects that have been mentioned are analgesic effects, interference with the activity of certain metalloproteinases and neuropeptides that are implicated in pain, and prevention of the destruction of bone by tumors. Gallium maltolate is being investigated for use/treatment in bladder cancer, lymphoma (unspecified), multiple myeloma, paget's disease, and prostate cancer.

PERFLUBRODEC is a component of an artificial perfluorochemical-based oxygen carrier OXYGENT. Using solely 3.6%w/v egg yolk phospholipid, Alliance Pharmaceutical Corporation (San Diego, California, USA) developed a concentrated (60% w/v) and stable perfluorocarbon emulsion, OXYGENT, which is composed of 58% w/v perfluorooctyl bromide and 2% w/v perfluorodecyl bromide, with an average particle size of 0.16-0.18 μm diameter. As a blood substitute OXYGENT has been administered to patients undergoing surgeries in clinical trials, however development was discontinued.

Metesculetol (permethol) is a vitamin P derivative. It increases capillary resistance and reduces membrane permeability. Permethol is for damaged gums and helps to stop gum bleeding, relieves inflammation and nourishes the gum tissues. It is used as a component of products for oral cavity care.