Prostamedix is a 68Ga-labeled ligand of the prostate-specific membrane antigen (PSMA) for Prostate Cancer PET imaging. Because of the increased expression of PSMA in Prostate Cancer and its metastases, Prostamedix was reported to exhibit a favorable lesion-to-background ratio with high detection rates. Further studies evaluating Prostamedix showed substantially higher detection rates in patients with recurrent PC than reported for other imaging modalities, especially at low PSA values. The chelator HBED-CC (N,N'-bis-[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N'-diacetic acid), represents a hitherto rarely used acyclic complexing agent especially allowing efficient radiolabelling with 68Ga even at ambient temperature. By combining HBED-CC with the PSMA inhibitor Glu-urea-Lys, a favorable aromatic part is introduced into the radiotracer which was found to be a necessary requirement for sustainable interaction with the PSMA receptor, putatively with the accessory hydrophobic pocket of the PSMA

Setmelanotide (RM-493), is an investigational, first-in-class melanocortin-4 receptor (MC4R) agonist in development for the treatment of rare genetic disorders of obesity. Setmelanotide is thought to activate the MC4R, part of a key biological pathway in humans that regulates weight by increasing energy expenditure and reducing appetite. Variants in genes within the MC4 pathway are associated with unrelenting hunger, known as hyperphagia, and severe, early-onset obesity. Setmelanotide is a potential replacement therapy that may restore lost activity in the MC4 pathway, reestablishing weight and appetite control in patients with these rare genetic disorders.

Gallium edotreotide Ga-68 is a radioconjugate consisting of the octreotide derivative edotreotide labeled with gallium 68 (Ga-68). Similar to octreotide, gallium Ga 68-edotreotide binds to somatostatin receptors (SSTRs), especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells and their metastases, thereby allowing for imaging of SSTR-expressing cells with positron emission tomography (PET). Gallium edotreotide Ga-68 has been authorized in the EU as SomaKit for the diagnosis of gastro-entero-pancreatic neuroendocrine tumors. It was investigated in clinical trials for imaging of brain tumors, pituitary tumors and neuroendocrine tumors of various origin.

Bremelanotide (formerly PT-141) was developed for the treatment of female sexual dysfunction, hemorrhagic shock, and reperfusion injury. Bremelanotide, a synthetic peptide analog of α-melanocyte-stimulating hormone (α-MSH) is an agonist at melanocortin receptors including the MC3R and MC4R, which are expressed primarily in the central nervous system. Bremelanotide originally was tested for intranasal administration in treating female sexual dysfunction but this application was temporarily discontinued in 2008 after concerns were raised over adverse side effects of increased blood pressure. It appears that development for hemorrhagic shock and reperfusion injury has been discontinued. Palatin Technologies licensed North American development and commercialization rights of bremelanotide to Amag in January 2017. In June 2018, the US Food and Drug Administration (FDA) accepted AMAG Pharmaceuticals’ new drug application for bremelanotide for treatment of hypoactive sexual desire disorder in premenopausal women. If approved, bremelanotide will be available as a self-administered, disposable subcutaneous auto-injector used in anticipation of a sexual encounter.

Afamelanotide (SCENESSE) is a synthetic α-melanocyte stimulating hormone analog and first-in-class melanocortin-1 receptor agonist that is approved in the EU for the prevention of phototoxicity in adults with erythropoietic protoporphyria. Afamelanotide differs from endogenous α-melanocyte stimulating hormone at the fourth and seventh amino acid residues, increasing its resistance to immediate degradation and increasing its binding time to melanocortin-1 receptor. Afamelanotide is mimic the pharmacological activity of α-melanocyte stimulating hormone by binding to the melanocortin-1 receptor on melanocytes and activating the synthesis of eumelanin. Eumelanin provides photoprotection through mechanisms including, but not limited to, the absorption and scattering of visible and UV light and antioxidant activity. Afamelanotide increases eumelanin density in healthy volunteers and patients with erythropoietic protoporphyria. In healthy, fair-skinned volunteers, a significant increase in melanin density and skin darkening in both sun-exposed and non-sun-exposed sites was seen with subcutaneous injections of afamelanotide. The most common afamelanotide adverse events included headache and nausea. Common adverse effects include back pain, upper respiratory tract infections, decreased appetite, migraine, and dizziness.

Fluorodopa F-18 is the amino acid analog fluorodopa (FDOPA) labeled with fluorine F 18, a positron-emitting isotope. It is diagnostic PET agent, which has been used for decades in imaging the loss of dopaminergic neurons in Parkinson's disease, and more recently to detect, stage and restage neuroendocrine tumours and to search for recurrence of viable glioma tissue. Fluorodopa F-18 is able to cross the blood-brain barrier and is taken up by brain tumor cells. As uptake is higher in tumor cells, tumors may then be imaged using positron emission tomography (PET). Assessing tumor uptake of FDOPA may be beneficial for diagnosis, localization and in determining further treatment. The clinical usefulness of Fluorodopa F-18 has been evaluated and recognised in France and subsequently in several EU countries. Fluorodopa F-18 was registered in France in 2006. 6-fluoro-(18F)-L-3,4-dihydroxyphenylalanine (FDOPA) is a large, neutral amino acid that is transported into presynaptic neurons, where it is converted by the enzyme aromatic aminoacid decarboxylase [AAAD]) into fluorodopamine-(18F), which subsequently enters cathecholamine-storage vesicles. 6-fluoro(18F)-L-dopa crosses the blood-brain barrier; therefore, when injected into the blood stream, it reaches the dopaminergic cells in the brain and is used by the brain as a precursor for dopamine. This makes it possible to monitor intracerebral synthesis and uptake of dopamine by means of the positron-emitting 6-fluoro(18F)-L-3,4-dihydroxyphenylalanine (FDOPA), in conjunction with externally-placed devices suited for detection of annihilation photons, which progressively led to the most recent positron emission tomography (PET) units. Iasodopa, the commercial preparation of FDOPA that obtained a marketing authorisation in France in November 2006 (which is currently recognised by several other EU countries), is a solution for injection. The activity available at time of administration ranges from 0.1 GBq to 0.8 GBq per vial. The half-life of the radionuclide is 109.8 min with emission of positron radiation (Emax: 0.633 MeV) followed by photon annihilation radiations of 0.511 MeV.

Ivosidenib (AG-120) is an inhibitor of isocitrate dehydrogenase 1 (IDH1) This experimental drug inhibits mutant IDH1, leading to increased differentiation and decreased proliferation in IDH1 positive tumors and thus is thought to be promising for the treatment of IDH1-mutated tumors. In vivo treatment with AG-120 of TF-1 cells, primary human AML patient samples expressing mutant IDH1 and primary human blast cells cultured ex vivo showed that AG-120 is effective at lowering 2-HG levels and restoring cellular differentiation. It showed promising results in a phase I trial in patients with relapsed or refractory acute myeloid leukemia and is being evaluated in Phase III in previously-treated subjects with nonresectable or metastatic cholangiocarcinoma with an IDH1 mutation.

Lutetium Lu 177 dotatate binds to somatostatin receptors with highest affinity for subtype 2 receptors (SSRT2). Upon binding to somatostatin receptor expressing cells, including malignant somatostatin receptor-positive tumors, the compound is internalized. The beta emission from Lu 177 induces cellular damage by formation of free radicals in somatostatin receptor-positive cells and in neighboring cells. LUTATHERA® (lutetium Lu 177 dotatate) is indicated for the treatment of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), including foregut, midgut, and hindgut neuroendocrine tumors in adults.

Plazomicin is a novel aminoglycoside antibiotic that binds to the bacterial 30S ribosomal subunit, thus inhibiting protein synthesis in a concentration-dependent manner. Plazomicin displays a broad spectrum of activity against aerobic gram-negative bacteria including extended-spectrum β-lactamase-producing Enterobacteriaceae, carbapenem-resistant Enterobacteriaceae, and organisms with aminoglycoside-modifying enzymes. Plazomicin resistance in Enterobacteriaceae is via modification of the ribosomal binding site due to expression of 16S rRNA methyltransferases. ZEMDRI (plazomicin) injection for intravenous use is indicated for the treatment of patients 18 years of age or older with Complicated Urinary Tract Infections (cUTI) including Pyelonephritis.

Deflazacort is a glucocorticoid developed for the treatment of different inflammatory and immune conditions. The drug is rapidly metabolized to an active metabolite, 21-hydroxy-deflazaxort that may cross the blood brain barrier. Deflazacort acts by suppressing inflammatory response.