L778123 Cancer Drug: Uses, How it Works, Dosage, Efficacy, Side Effects

What is L778123 cancer drug?

L778123 cancer drug is a peptidomimetic farnesyl protein transferase (FPTase) inhibitor. L778123 cancer drug is currently being studied as intravenous formulations against a variety of cancers. The cost of cancer drug development can reach billions and the process typically takes 8–10 years from discovery to registration.

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How L778123 cancer drug works

L778123 anticancer drug belongs to the family of drugs called enzyme inhibitors. It may inhibit the transformation of normal cells into cancer cells. This drug is said to inhibit signaling pathways for tumor cell growth and proliferation. Intra- or inter-cellular communication disorders are a major cause of pathogenic mechanisms. Protein phosphorylation is one of the most significant signal transduction mechanisms by which inter-cellular signals regulate crucial intra-cellular processes such as ion transport, cellular proliferation and differentiation, and hormone responses.

L-778123 was designed to selectively compete with the binding of the CAAX (a group of proteins with a specific amino acid sequence at C-terminal that directs their post-translational modification) fragment of Ras in Protein farnesyltransferase (FTase) which catalyzes the attachment of a farnesyl lipid group to the cysteine residue located in the C-terminal tetrapeptide of many essential signal transduction proteins, including members of the Ras superfamily.

Drug Administration

During the phase I clinical trials, L-778123 was provided by Merck Research Laboratories (West Point, PA) as a 10 or 50 mg/ml solution for i.v. infusion and it was stored at 2 to 8°C. L-778123 was diluted with normal saline to fill reservoirs of 100 to 1000 ml, depending on the dose level, and administered as a 7-day continuous i.v. infusion with a Deltec CADD-PLUS infusion pump at a minimum infusion rate of 3.8 ml/h. Because diluted solutions of L-778123 are stable for 1 week at 25°C, a maximum supply of 3 days was prepared at once.

Efficacy of L-778123

L-778123 is a dual inhibitor of Farnesyl Protein Transferase (FPTase) and Geranylgeranyl Protein Transferase type-I (GGPTase-I), which can completely inhibit Ki-Ras prenylation. L-778123 has been used in phase I clinical trials to determine its effectiveness in treating patients with recurrent or refractory solid tumors. L-778123 was also studied in combination with paclitaxel to determine efficacy as a treatment for both recurrent or refractory solid tumors, and lymphomas.

Side effects

L778123 cancer drug is a drug in development and the side effects are currently unknown. Drug development process, from discovery to market, is long and costly. Rigorous processes are in place during clinical trials that protect the safety of study participants and also ensure that the collection of adverse event data is complete. This completeness, coupled with the randomized design, also helps develop an understanding of the benefits and side effects of a new medicine by strengthening the validity of the comparisons between the new drug and the comparator, which could be a placebo or an active therapy for the condition under study.

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