Echinomycin is a cyclic peptide of the family of quinoxaline antibiotics that was originally isolated from Streptomyces echinatus. It is thought to act as a bifunctional DNA intercalator. Echinomycin has a binding site size of four base pairs. The strong binding sites for echinomycin contain the central two-base-pair sequence 5'-CG-3'. Echinomycin interferes with HIF-1 DNA binding in a sequence-specific fashion. It was brought into clinical trials by the NCI 20 years ago based on its antitumor activity. It has been extensively tested in phase I-II clinical trials. Nausea, vomiting, reversible liver enzyme abnormalities, and allergic reactions were the most common toxicities encountered. However, minimal or no antitumor activity was found in phase II clinical trials.

MK-6186 is a novel nonnucleoside reverse transcriptase inhibitor (NNRTI) which displays subnanomolar potency against wild-type (WT) HIV virus and the two most prevalent NNRTI-resistant RT mutants (K103N and Y181C) in biochemical assays. In addition, it showed excellent antiviral potency against K103N and Y181C mutant viruses. In 2010 MK-6186 was studied in phase I clinical trials but no further development reports were published.

Praziquantel, (-)- is oxopyrazinoisoquinoline derivative and a levorotated isomer of Praziquantel patented by Merck Patent G.m.b.H. as anthelmintics agent. In rabbits infested with S. japonicum, the therapeutic effect of Praziquantel, (-)-was greater than that of dl-praziquantel as rated by the number of the worms in tissues and by liver damage. Histopathological examination showed that liver egg granulomas in the levo-praziquantel group were fewer in no. and smaller in size and were predominantly composed of Pseudotubercles instead of eosinophilic abscesses. Levo-praziquantel is therapeutically superior to praziquantel, while dextro-praziquantel is almost ineffective.

Piprocurarium is a curarimimetic. It is antagonized by neostigmine. Piprocurarium is strongly vagolytic, producing tachicardia. Its duration of action is shorter than that of d-tubocurare and longer than that of succinylcholine. Piprocurarium is not hypotensive, is only slightly histaminogenic, is nonirritating to the veins, and can be mixed with all the anesthetic drugs. Piprocurarium has been offered for clinical trial as a brief-acting, nondepolarizing neuromuscular blocking drug. The drug appears to be anything but short acting. A persistent tachycardia and elevation in systolic and diastolic pressure invariably follows its intravenous injection. Alarming electrocardiographic changes occur, characterized by AV dissociation, depression of the ST segment, supraventricular tachycardia and, at times, inversion of the T waves. In view of these circulatory effects, it is doubtful that the drug will be useful clinically.

5-(hydroxymethyl)-2-furaldehyde (5-Hydroxymethyl-2-furancarboxaldehyde, 5‐hydroxymethyl‐2‐furfural) is found in garden onion. It is obtainable from various carbohydrates. 5-Hydroxymethyl-2-furancarboxaldehyde is present in tomatoes, tobacco oil etc. It is a constituent of numerous plant species. 5-Hydroxymethyl-2-furancarboxaldehyde is used as an index of heat treatment and deterioration in food such as tomato paste, honey and fruit juices. Also an indicator of adulteration with acid-converted invert sugars. The heterocyclic aldehyde 5‐hydroxymethyl‐2‐furfural (5HMF, Aes‐103, BAX 555) interacts allosterically with the abnormal form of haemoglobin (Hb), HbS, in red blood cells (RBCs) from patients with sickle cell disease (SCD), thereby increasing oxygen affinity and decreasing HbS polymerization and RBC sickling during hypoxia. 5HMF markedly reduced the deoxygenation-induced dehydration of RBCs whether in response to maintained deoxygenation or to cyclical deoxygenation/re-oxygenation. 5HMF was found to inhibit Psickle, an effect which correlated with its effects on sickling. Deoxygenation-induced activation of the Gardos channel and exposure of phosphatidylserine were also inhibited, probably indirectly via reduced entry of Ca(2+) through the Psickle pathway. Effects of 5HMF on KCC were more modest with a slight inhibition in N-ethylmaleimide (NEM, 1 mm)-treated RBCs and stimulation in RBCs untreated with NEM. These findings support the hypothesis that 5HMF may also be beneficial through effects on RBC ion and water homeostasis. AesRx is developing Aes-103 as an orally bioavailable, chronic therapy for SCD. Aes‐103 is currently in phase II clinical trials in SCD patients in the USA and UK. Aes-103 has received orphan designation from the US Food and Drug Administration and is eligible for orphan status in Europe.

Icaritin is a monoprenylated favonol with 4′-methoxyl from Epimedium Genus. It has been documented to have osteoblastic and neuroprotective activities. It can reduce the incidence of steroid-associated oesteonecrosis in rabbit with inhibition of both intravascular thrombosis and extravascular lipid deposition for maintaining the integrity of intraosseous vasculature. Icaritin shows anti-infammatory activity and inhibitory activities against cancer cells. The phase III clinical trial is planned for the treatment of Hepatocellular carcinoma.

Relamorelin (also known as BIM28131 or RM-131) is a synthetic, selective, prokinetic ghrelin analog that was developed for treatment of gastrointestinal motility disorders (such as chronic constipation and diabetic gastroparesis). Relamorelin was shown to relief symptoms such as nausea, fullness, bloating and abdominal pain. It is safe and well-tolerated in healthy individuals, and has no neurological or cardiovascular adverse effects, making this a promising drug with an advantage over other available therapies. A phase III clinical trial comparing the efficacy of relamorelin with that of placebo in participants with diabetic gastroparesis (DG) was still ongoing in 2019.

DCFBC F-18 is a radioconjugate containing a low molecular weight tracer, DCFBC, specific for prostate-specific membrane antigen (PSMA) and labeled with the positron-emitting isotope fluorine F 18 with potential prostate tumor imaging upon positron emission tomography (PET). Upon administration, the DCFBC moiety of fluorine F 18 DCFBC specifically targets and binds to the tumor-associated antigen PSMA, thereby allowing the visualization of tumor cells expressing PSMA upon PET. F 18 DCFBC is investigated in phase 2 clinical trials in patients with prostate cancer.