BX 471 is an oral nonpeptide chemokine receptor1 (CCR1) antagonist that was under clinical development with Bayer Healthcare Pharmaceuticals (formerly Bayer Schering Pharma AG and Berlex) for the treatment of various inflammation-related disorders, including endometriosis. The CCR1 antagonist was also thought to have potential application in diagnostic imaging, particularly as an imaging biomarker for the diagnosis of Alzheimer's disease. Berlex initiated the development of the radiolabelled small molecule CCR1 antagonist, BX 471, for a specific diagnostic test for both early detection and for tracking disease progression following the discovery that the CCR1 protein was found in the brains of patients with Alzheimer's disease, and that increased levels of this protein were correlated with advancement of the disease. However, development of the agent for diagnostic imaging appears to have been discontinued. BX 471 was also in development for the treatment of autoimmune diseases, including multiple sclerosis and psoriasis; however, development in these indications, as well as multiple myeloma and endometriosis, also appears to have been discontinued. A phase II study of BX 471 in endometriosis had been completed.

PF-04531083 is selective Nav1.8 blocker. It has been investigated for the treatment of chronic pain, heart pain, post-surgical dental pain. However, these trials were discontinued.

GlaxoSmithKline (GSK) was developing GSK-239512 as a histamine H3 receptor antagonist/inverse agonist as a monotherapy treatment for subjects with mild-to-moderate probable Alzheimer's disease (AD), multiple sclerosis and Schizophrenia. However, in March 2017, GSK globally discontinued the study of GSK-239512 at phase II.

Meisoindigo ((E)-1,1'-dimethyl-[3,3'-biindolinylidene]-2,2'-dione) is a derivative of Indigo Naturalis, that has been used in China for chronic myeloid leukemia. In vitro cell line studies have shown that this agent might induce apoptosis and myeloid differentiation of acute myeloid leukemia (AML). Meisoindigo has been a routine therapeutic agent in the clinical treatment of chronic myelogenous leukemia (CML) in China since the 1980s. In phase III clinical trial of Meisoindigo involving 402 patients, it was shown that Meisoindigo was equally efficient for both newly diagnosed and previously treated CML patients after oral administration. The hematological complete response (CR) and partial response (PR) rates, respectively, were 45.0 and 39.3% for newly diagnosed patients and 35.9 and 41.4% for previously treated patients. Meisoindigo was generally well tolerated. The most frequent side‑effects were bone, joint and/or muscle pain of varying degrees when the dosage was more than the suitable one.

Tradipitant is a neurokinin 1 receptor antagonist. The dose of 50 mg of tradipitant given orally for 4 weeks was not superior to placebo in reducing itch intensity in patients with atopic dermatitis. However, in a subsequent study, in which a higher dose (85 mg) was administered for 8 weeks, significant antipruritic effect compared with placebo was recorded. Tradipitant is in phase III clinical trial for the treatment of atopic dermatitis and gastroparesis. Vanda Pharmaceuticals plans a phase III trial in Motion Sickness in 2019.