Monday, March 19, 2012

In hope for a wild card. A coming decade in development of anticancer treatment. Forecast.

I have found very interesting review of the situation with oncology products development. The information is very compact and concrete. I sincere recommend reading it for those who works with drug development process.  

Here is my comments:

Numbers are impressive:

Currently, there are over 725 anticancer drugs in clinical development and at least another 300-500 in preclinical and research stages. Over 3,500 novel approaches have been evaluated clinically or preclinically in the last decade. Currently, more than 10,000 clinical trials with novel and approved agents, alone or in combination, are ongoing with over 12% having entered phase III status. Globally, over 1,000 distinct commercial entities are developing oncology drugs or have technologies applied to this sector

Not bad. Nobody knows how many of these drugs will pass the Death Valley but the amount of the candidates is huge!

Several hundred cancer-related targets have been identified and over 160 distinct have been evaluated in clinical trials but few of these efforts led to commercialized products, with none providing a bona fide 'cure'. Currently, over 210 novel targeted agents are being evaluated in phase I clinical trials, and many have entered phase III trials.

Well, it looks like we have an understanding of the value of targeted approach. Do we have anything else? Actually yes:

Patient selection based on verified tumors' molecular profile, personalized medicine, and advances based on in vitro testing (IVT)… The IVT sector has grown exponentially in the last decade. Over 250 companies are developing some type of IVT in cancer. IVT include screening tests, diagnostics, pharmacogenomics, prognostics, disease monitoring tests, theragnostics, toxicogenomics, etc. For instance, over 30 companies have development programs in IVT in ovarian cancer, 42 in lung cancer, 19 in bladder cancer, etc.

Not everyone works with targeting and with HTS! This is a positive moment. Anything else? Yes:

Trials combining novel targeted agents

Targeted agents currently constitute the majority of novel drugs entering clinical trials. Over 200 novel targeted drugs are in phase I clinical trials, mostly small molecule protein kinase inhibitors or monoclonal antibody (MAb)-based blockers of cell surface receptors. These newer agents are addressing over 160 distinct molecular moieties shown to play a role in malignancy. Novel targeted agents are usually evaluated as monotherapies or in combination with approved/marketed agents. It is anticipated that in this decade, such agents will also be clinically evaluated in combinations with each other. Such an endeavor will take clinical development to a new level of complexity but may also have surprisingly beneficial results.

MAbs – also targeted therapies. Fine. But note that MAbs usually used in a combination with proved chemotherapy. Why? It is another subject for discussion. 

Currently, over 130 MAb-based agents are in clinical development with 20 having entered phase III clinical trials.

We say nothing here about the cost of these drugs. Do we have something else? Yes, very mechanistic and creative with magic-bullet ambition – antibody-drug conjugates:

 Antibody engineering technologies and novel immunoconjugates, radioimmunoconjugates, fusion proteins, and antibody-drug conjugates (ADC)

Monoclonal antibodies (MAb) are the backbone of the oncology drug sector. No fewer than 125 companies are focusing in oncology applications of MAb in this ever advancing field. The attractiveness of MAb is their ability to target surface receptors with exquisite specificity and also, in many cases, stimulate the immune system to destroy cells expressing such receptors. In the past decade over 650 distinct MAb have been evaluated in oncology. Although effective as signal transaction inhibitors on their own, the targeted specificity of MAb makes them excellent ferries of drugs/toxins, and radioisotopes to cancer cells. Such an application of MAb is currently exploited in antibody drug conjugates (ADC), a burgeoning area of drug development with 11 drugs in clinical trials with one in phase III.

The idea is very “sexy” – let’s just wait for the first results in coming years!

Next we have something less targeted:

Immunotherapies/vaccines

Although the human immune system is capable of raising an immune response against many cancer types, it fails to eradicate cancer in most patients, possibly because of negative regulation of the immune system by the tumor. Immune surveillance is the major mechanism by which malignant cells are recognized and eliminated by the immune system before they can develop into clinically detectable tumors. Although, immune system failure may contribute to the survival and proliferation of cancer cells, it is now theorized that tumors adopt ways for evading eradication by the immune system. After several failures of cancer immunotherapies in late phase trials, interest has been rekindled in this area by several positive developments, primarily by favorable results with Dendreon's prostate vaccine Provenge. Over 125 immunotherapeutics/vaccines are in clinical development, with many demonstrating favorable activity with low toxicity.

We have to wish good luck! Vaccination has eradicated a lot of dangerous diseases – hopefully vaccines will help us to treat cancer!

A real non-targeted and fresh approach:

Oncolytics/virotherapy approaches

After many years in development virotherapy is beginning to show effectiveness in the clinic. As many 32 distinct oncolytics have been investigated over the last 10 years with 11 agents currently in clinical development in various cancer indications.

Very interesting! Hopefully we can get a real “wild card” here… I have to check it closely!

Then we still have a “classical approach” – proven strategy which helped to develop a majority of blockbusters:

Novel cytotoxics

Cytotoxics remain the backbone of cancer treatment for both advanced disease and in adjuvant and neoadjuvant settings. Nearly every approved and most novel agents are being combined with a cytotoxic regimen. Therefore, considerable effort is dedicated to improving every aspect of cytotoxic chemotherapy. In the past decade over 663 distinct cytotoxics were evaluated preclinically and clinically with 228 currently under development; 98 incorporate some type of a delivery system and 32 are prodrugs. Among 195 currently in clinical development, 32 novel agents have entered phase III clinical trials. Many clinical programs involve approaches to improve the performance and reduce the non-specific toxicity of leading marketed chemotherapeutics as well as of several experimental drugs that were withdrawn from development because of unacceptable toxicity and formulation difficulties.

What else? Drug delivery!

Advances in drug delivery, including nanotechnology

Drug delivery is the second most important challenge of targeted therapeutics after proof of efficacy in vitro and in vivo, and perhaps one of the key reasons drugs that perform well in small animals models fail in humans. New therapeutic approaches such as microRNA inhibitors reignited the quest for effective drug delivery systems. Nanotechnology is currently the holy grail of drug delivery in oncology being pursued by 40 distinct entities, each developing its own version of this promising approach, which may revitalize the cytotoxic drug sector that is still the standard treatment for almost all types of advanced disease and enable the clinical application of such novel technologies as RNA interference (RNAi).

Sure! Inclusive nanotechnology! How else?

We can see that all approaches could be roughly divided in two categories:

·         Molecular targeting approaches (small molecules and MAbs) – automated based on HTS, genomics, proteomics etc

·         Non-molecular targeting approaches – creative, original and non-trivial

In general I could judge the situation as optimistic – not every product is based on concept of molecular targeting paradigm.

Basically I think that in a coming decade (2012-2022) molecular targeting approaches will be less popular and we will see a lot of disappointed failures in their clinical trials programs. Simultaneously we hopefully will experience emerging of a promising drug delivery solutions, virotherapeutic or totally novel approaches which will be able to revolutionize cancer treatment. However I doubt that modern paradigm will be replaced – it is so inert that it can take a couple of generation’s work to completely discard the targeting “key-lock” paradigm.

No comments:

Post a Comment