Neratinib (HKI-272) is a pan-HER inhibitor, this irreversible tyrosine kinase inhibitor binds and inhibits the tyrosine kinase activity of epidermal growth factor receptors, EGFR (or HER1), HER2 and HER4, which leads to reduced phosphorylation and activation of downstream signaling pathways. Neratinib is a modified form of the discontinued compound pelitinib, and was originally being develoAdditionally, phase II development of oral neratinib as a neoadjuvant therapy for breast cancer, as a second-line therapy for non-small cell lung cancer, and for other solid tumours is also in progress in numerous countries worldwide. ped by Wyeth (later Pfizer). Oral neratinib is awaiting approval as an extended adjuvant therapy for breast cancer in the EU and in the US. Blocking HER2 function by a small molecule kinase inhibitor, such as neratinib, represents an attractive alternate strategy for the growth inhibition of HER2-positive tumours.

Potassium citrate is indicated for the management of renal tubular acidosis with calcium stones, hypocitraturic calcium oxalate nephrolithiasis of any etiology, uric acid lithiasis with or without calcium stones. WhenPotassium citrate is given orally, the metabolism of absorbed citrate produces an alkaline load. The induced alkaline load in turn increases urinary pH and raises urinary citrate by augmenting citrate clearance without measurably altering ultrafilterable serum citrate. Thus, potassium citrate therapy appears to increase urinary citrate principally by modifying the renal handling of citrate, rather than by increasing the filtered load of citrate. Potassium citrate is used as a food additive (E 332) to regulate acidity.

Epelsiban (GSK557296), a pyridyl-2,5-diketopiperazine, is a potent, highly selective, and orally bioavailable non-peptide oxytocin receptor antagonist. GlaxoSmithKline was developing epelsiban for the treatment of women infertility due to adenomyosis and premature ejaculation.

Merotocin (FE-202767 or carba-1-[4-FBzlGly(7)]dOT) is a selective peptidic oxytocin receptor agonist. It is currently in clinical development for the treatment of preterm mothers requiring lactation support.

PF-3274167 (Cligosiban) is a potent, selective, brain penetrant oxytocin receptor antagonist. Cligosiban interrupts the expulsion phase of ejaculation by reducing the normal bulbospongiosum burst pattern and reducing the expulsions that accompany bursts. Cligosiban represents a promising compound to test the clinical hypothesis that antagonism of central oxytocin receptors may be of therapeutic benefit in the treatment of premature ejaculation. [11C]PF-3274167 is not a suitable tracer for imaging of OTR in rat brain, probably because of a too low affinity for this receptor in addition to a poor brain penetration. PF-3274167 had been in phase I clinical trial for the treatment of sexual function disorders and urinary incontinence. However, this research has been discontinued.

Erlosiban (OBE-001 or Nolasiban) is an oral oxytocin receptor antagonist. Erlosiban inhibits myometrium contractions and inflammation elicited by oxytocin. Erlosiban has the potential to decrease contractions and improve uterine blood flow hence enhancing the receptivity of the endometrium to embryo implantation. This may increase the rates of successful implantation, clinical pregnancy, and live-births among patients undergoing ART, or more specifically IVF procedures.

Barusiban, a long-acting oxytocin antagonist, has been studied to stop preterm labor in pregnant women at late gestational age. The experiments failed to demonstrate the effectiveness and were discontinued. However, barusiban participates in phase II clinical trials for female infertility.

Retosiban is a small molecule oxytocin receptor antagonist that is under evaluation for treatment of premature labor. Retosiban was found to be safe in healthy non-pregnant volunteers in phase I studies. Intravenous retosiban also had good safety and tolerability in phase II studies and was suggested to prolong pregnancies in women with preterm labor. Phase III studies have been conducted to demonstrate the efficacy of retosiban to prolong pregnancy and improve neonatal outcomes, and compare effects with a similar drug atosiban, but these studies were terminated in 2018 (not due to adverse events).

WAY 267464 dihydrochloride is a potent and selective agonist at the oxytocin receptor (OTR). WAY 267464 has been shown to cross the blood-brain-barrier to a significantly greater extent than exogenously applied oxytocin. WAY 267464 dose-dependently reduced anxiety on the four-plate test and prevented the deficits in prepulse inhibition induced by MK-801 or amphetamine. The ability of WAY 267464 to function as a V1AR antagonist may limit its potential therapeutic use in humans, as it would conceivably prevent the improvements in social behavior and social cognition that may be assumed to arise from a primary OTR agonist action.

TC OT 39 was developed as potent non-peptide oxytocin receptor partial agonist and V2 vasopressin receptor agonist. Also was a V1a vasopressin receptor antagonist.