The monoaminergic system consists of a dynamic network of neurons located in the brainstem with widely branches ensuring the monoamine neurotransmitters act in most part of the brain. The monoamine neurotransmitters, dopamine, noradrenaline, and serotonin play a pivotal role in many important physiological functions including attention, mood, motivation, pain sensation, arousal, and sexual function. The levels of monoamines can be regulated in the synaptic cleft by inhibition of monoamine transporters or by inhibition of the degradation with monoamine oxidase inhibitors. Medications with these properties are used to treat depression, attention deficit hyperactive disorder (ADHD), narcolepsy, anxiety, pain, and Parkinson´s disease. Several of these medications have improved the treatment of the diseases, but may also be associated with lack of effect in a fraction of patients and with adverse effects. To address the unmet need and to avoid adverse effects, Initiator Pharma A/S has developed a series of inhibitors of monoamine transporters (MATs) with unique profiles for the three monoamine transporters of dopamine, noradrenaline, and serotonin and an attractive safety profile. The different profiles of the drug candidates for inhibition of the MATs in our pipeline allow targeting specific diseases, e.g., so far erectile dysfunction of organic origin, erectile dysfunction of psychogenic origin caused by depression, low mood or anxiety – or caused by the pharmacological therapies these patients receive), and pain (Trigeminal neuralgia).