Metenkephalin (Met-enkephalin) is an endogenous opioid peptide that acts as an agonist at μ-opioid receptors (μORs) and δ-opioid receptors (δORs). Met-enkephalin exhibits neuromodulatory, antinociceptive/analgesic, antidepressant, and gastrointestinal motility modulating activities. Like other endogenous opioids, met-enkephalin modulates expression of opioid receptors and plays a role in reward/reinforcement signaling. Met-enkephalin is also involved in exercise-induced reversal of neuropathic pain and in animals undergoing the forced swim test, decreases immobility time. Met-enkephalin inhibits gastrointestinal muscle contractility, inhibiting motility and gastric emptying. Additionally, analogs of this peptide display anticancer and antiepileptic/anticonvulsant activities.

MPC-3100 is a fully synthetic, orally bioavailable, Hsp90 inhibitor developed by Myriad Pharmaceuticals, Inc for cancer treatment. MPC-3100 targets the N-terminal ATP-binding site of Hsp90 and blocks the activity of ATPase. MPC-3100 shows a broad spectrum anti-proliferative activity against various cancer cell lines, such as HCT-116, NCI-N87 and DU-145. MPC-3100 also inhibits tumor growth in the NCI-N87 gastric cancer xenograft mode. Moreover, pharmacokinetics studies show that MPC-3100 displays a superior oral pharmacokinetics profile, good overall exposure and a reasonable hepatic clearance rate. Phase I clinical studies demonstrate MPC-3100 is safe and tolerated when administered at doses below 600 mg per day

MPC-3100 is a fully synthetic, orally bioavailable, Hsp90 inhibitor developed by Myriad Pharmaceuticals, Inc for cancer treatment. MPC-3100 targets the N-terminal ATP-binding site of Hsp90 and blocks the activity of ATPase. MPC-3100 shows a broad spectrum anti-proliferative activity against various cancer cell lines, such as HCT-116, NCI-N87 and DU-145. MPC-3100 also inhibits tumor growth in the NCI-N87 gastric cancer xenograft mode. Moreover, pharmacokinetics studies show that MPC-3100 displays a superior oral pharmacokinetics profile, good overall exposure and a reasonable hepatic clearance rate. Phase I clinical studies demonstrate MPC-3100 is safe and tolerated when administered at doses below 600 mg per day

Pexiganan is a 22-amino-acid synthetic cationic peptide. It is an analog of magainin 2, which is a host defense peptide isolated from frog skin. The drug is thought to act by disturbing the permeability of the cell membrane or cell wall. Pexiganan exhibited in vitro broad-spectrum antibacterial activity when it was tested against 3,109 clinical isolates of gram-positive and gram-negative, anaerobic and aerobic bacteria. It is currently in phase 3 clinical trials as a topical antimicrobial agent for the treatment of mild infections associated with diabetic foot ulcers. In vitro data for pexiganan acetate suggest that the drug does have hemolytic activity at concentrations relevant for antibacterial activity. In association with tigecycline, pexiganan administration could overcome antibiotic resistance and increase the effectiveness of treatment against P. aeruginosa sepsis.

Elamipretide or SS-31 (D-Arg-2', 6'-dimethyltyrosine-Lys-Phe-NH2) is a mitochondria-targeted antioxidant. Elamipretide, is a peptide compound that readily penetrates cell membranes, and targets the inner mitochondrial membrane where it binds reversibly to cardiolipin. In preclinical or clinical studies, elamipretide increases mitochondrial respiration, improves the electron transport chain function and ATP production and reduces formation of pathogenic ROS levels. This elamipretide-cardiolipin association has been shown to normalize the structure of the inner mitochondrial membrane, thereby improving mitochondrial function. Functional benefit is achieved through improvement of ATP production and interruption and potential reversal of damaging oxidative stress. Stealth BioTherapeutics is investigating elamipretide in late stage clinical studies in three primary mitochondrial diseases—primary mitochondrial myopathy, Barth syndrome and Leber’s hereditary optic neuropathy – as well as an earlier stage clinical study in dry age-related macular degeneration.

METHYLENETETRAHYDROFOLIC ACID, L-(+), an endogenous biomodulator that was developed under the brand name modufolin or arfolitixorin by the Isofol Medical. Arfolitixorin is developed to increase the efficacy of standard of care chemotherapy for advanced colorectal cancer. This drug is currently being studied in a global phase 3 clinical trial. Besides, the drug successfully completed phase II as rescue therapy for osteosarcoma. 21 May 2019 Isofol Medical has received clinical patent protection for the arfolitixorinin USA. It relates to a method of increasing blood concentration of deoxyuridine, a blood biomarker for inhibition of tumor growth in human cancer treatment.

SPK-843 is a water-soluble partricin derivative patented by SPA Societa Prodotti Antibiotici S.p.A. and developed by Aparts and Kaken for the potential treatment of systemic fungal infections. In preclinical models, SPK-843 shows in vitro inhibitory activity comparable to or better than that of Amphotericin B against Candida spp., Cryptococcus neoformans, and Aspergillus spp. SPK-843 exhibits dose-dependent efficacy on murine pulmonary aspergillosis models. SPK-843 doses of higher than 1.0 mg/kg of body weight exhibit no renal toxicities and a tendency toward better survival prolongation than the estimated maximum tolerated doses of amphotericin B (Fungizone) and liposomal amphotericin B.