Properidine is an isopropyl analog of pethidine that acts as opioid analgesic.

Phenampromide is an opioid analgesic, which is considered to be structurally similar to isomethadone. Phenampromide belongs to the ampromide family of drugs, which also include propiram and diampromide. According to the literature, (R)-phenampromide has greater analgesic potency than its (S)-enantiomer. Synthetic narcotic analgesic phenampromide is under international control according to the UN Single Convention 1961 and its amendments, Schedule I.

Etisulergine (CQ 32-084) is an ergoline derivative. Etisulergine stimulates both dopamine D1- and D2-receptors, antagonizes alpha-adrenergic and serotonin 5-HT2 receptors. Etisulergine demonstrated antiparkinsonian activity in patients.

Betaprodine is an opioid analgesic under international control according to the UN Single Convention 1961. It has been used in obstetrics, as pre-operative medication, for minor surgical procedures.

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.

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.

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.

Anhydrovinblastine (AVLB) is a semisynthetic vinca alkaloid, which can safely be administered every 3 weeks at a dose of 21 mg/m2. Anhydrovinblastine is a cell cycle-specific anti-mitotic agent whose anti-tumour activity is directly related to its ability to bind tightly to tubulin and inhibit its polymerization into microtubules. Anhydrovinblastine has been used in trials studying the treatment of adult solid rumor, but this research has been discontinued.

Sanguinarine is an extract of the bloodroot plant Sanguinaria canadensis, a member of the poppy family. It is an inhibitor of protein phosphatases PP1, PP2C and PP2B in vitro. Also inhibits mitogen-activated protein kinase phosphatase-1 (MKP-1) and other enzymes. Sanguinarine exerts a protective effect in cerebral ischemia, and this effect is associated with its anti-inflammatory and anti-apoptotic properties. It was clinically tested as an agent against gingivitis and tooth plaques.