Sameridine was developed as a compound with both local anesthetic and opioid properties (partial micro-opioid receptor agonist). This drug participated in clinical trials when administered intrathecally to provide anesthesia for surgery and extended postoperative analgesia. However, further development of this drug was discontinued.

Halofuginone is a low molecular weight quinazolinone alkaloid, and a potent inhibitor of collagen alpha1(I) and matrix metalloproteinase 2 (MMP-2) gene expression. Halofuginone also effectively suppresses tumor progression and metastasis in mice. Halofuginone is a potent inhibitor of collagen a1(I) and matrix metalloproteinase 2 (MMP-2) gene expression. Halofuginone also suppresses extracellular matrix deposition and cell proliferation. Also was shown that halofuginone increased apoptosis in α smooth muscle actin- and prolyl 4-hydroxylase β-expressing cells in mdx diaphragm and in myofibroblasts, the major source of extracellular matrix. The profound antitumoral effect of halofuginone is attributed to its combined inhibition of tumour-stromal support, vascularization, invasiveness, and cell proliferation. HT-100 (delayed-release halofuginone), currently in clinical phase 1b/2a in five U.S. hospitals, is a small molecule drug candidate taken orally for the treatment of Duchenne muscular dystrophy (DMD) patients primarily through its ability to reduce fibrosis and inflammation and promote muscle fiber regeneration. The medicine candidate has been granted orphan drug designation in the U.S. and the EU — meaning it has been commercially undeveloped due to its limited profitability — and fast-track designation in the U.S. — an FDA process that aims to facilitate the development and patients’ reach to novel therapies for unmet medical needs.

Trimexiline is an antihistamine, venotonic agent.

Bristol-Myers Squibb developed BMS-184476 for the potential treatment of solid tumors. BMS-184476 participated in phase II clinical trials for patients with non-small-cell lung cancer, breast, and ovarian cancers. However, that development has been discontinued.

Vinformide (also known as N-formylleurosine), an N-formyl analog of leurosine possesses antineoplastic activity. This drug was studied for the treatment of lymphoma, leukemia and Hodkin’s disease. However, studies were discontinued, because vinformide exerted an acute cardiotoxic side effect.

Methylselenocysteine is a part of the mammalian physiology and is a well-tolerated, versatile and economical antiangiogenic agent. This compound participated in clinical trial to determine if vitamin supplementation with this compound could restore disruption of circadian rhythm in shift workers. The preclinical efficacy of methylselenocysteine has shown the combination of methylselenocysteine with androgen deprivation therapy can be useful for the treatment of advanced prostate cancer.

Vinleucinol (also known as vinblastine-isoleucinate or V-LEU) was developed as a vinca alkaloid derivative. This compound exhibited superior antitumor activity in malignant melanoma, small cell lung carcinoma, and breast cancer lines. Experiments on animals have shown that metabolite of vinleucinol was mainly responsible for the antitumor.

Oxiniacic Acid is a nicotinic acid derivative, that shows potent hypolipidemic activity.