Miltefosine is an anti-leishmanial agent. It is an alkyl phospholipids compound, was originally intended for breast cancer and other solid tumors. However, it could not be developed as an oral agent because of dose-limiting gastro-intestinal toxicity, and only a topical formulation is approved for skin metastasis. But Miltefosine showed excellent antileishmanial activity both in vitro and in experimental models. Miltefosine is effective in vitro against both promastigotes and amastigotes of various species of Leishmania and also other kinetoplastidae (Trypanosoma cruzi,T. brucei) and other protozoan parasites (Entamoeba histolytica, Acanthamoeba). Mechanism of action is unknown. It is likely to involve interaction with lipids (phospholipids and sterols), including membrane lipids, inhibition of cytochrome c oxidase (mitochondrial function), and apoptosis-like cell death. Miltefosine is approved for the treatment of Visceral leishmaniasis (due to Leishmania donovani), Cutaneous leishmaniasis (due to Leishmania braziliensis, Leishmania guyanensis, and Leishmania panamensis) and Mucosal leishmaniasis (due to Leishmania braziliensis).

Elbimilast or ronomilast (previously ELB 353) is a phosphodiesterase IV (PDE4) inhibitor. It has been investigated in the treatment of chronic obstructive pulmonary disease.

Elmustine (1-(2-hydroxyethyl)3-(2-chloroethyl)-3-nitrosourea or HECNU) is an alkylating agent with antineoplastic properties. Elmustine is monofunctional and bifunctional alkylating agent that form, in a quantitatively minor reaction, DNA-DNA crosslinks. In vitro, by far the most abundant alkylation products of DNA are those resulting from 2-hydroxyethylation. Elmustine is especially highly active against intracerebrally implanted tumors. It was in Phase II clinical trials for the treatment of glioma. Elmustine development has been discontinued.

Zindoxifene (D 16726 or 5-acetoxy-2-(4-acetoxyphenyl)-1-ethyl-3-methylindole), is an antiestrogenic phenylindole with a high affinity for the estrogen receptor. Zindoxifene exerts inhibiting activity against tumors of prostatic and mammary origins both in vitro and in vivo. It was in phase I/II study for the treatment of advanced breast cancer. Zindoxifene development has been discontinued.

Anpirtoline [D 16949] is a dichloropyridine derivative with antinociceptive and antidepressant activity. Anpirtoline has been described as an agonist at 5-HT1B and 5-HT1D receptors with a relatively high potency. It also acts as an agonist at 5-HT1A receptors, but has a lower potency than at the 5-HT1B sites. In addition, Anpirtoline acts as an antagonist at 5-HT3 receptors. The drug was in phase I clinical trials with ASTA Medica in Germany for the treatment of pain and depression, but development was suspended.