This write-up is based on some of the drugs
mentioned in the white paper: Productive Innovation Index (PII) 2015, celebrating the
top 30 pharmaceutical companies - most successful at bringing innovations to
market. Idea Pharma has produced this
white paper - this company www.ideapharma.com
links with pharma companies to successfully take new pharma products to market
(Idea Pharma is a phase 2 player). Idea
Pharma does work from phase 2a, for strategic positioning, differentiation,
value preposition, path to market strategy and so on…In phase 2 stage of
clinical trials, the molecule is tested on larger number of patients (100 to
300 nos.) for efficacy and safety.
The productive innovation index 2015 was topped by Johnson and Johnson.
In 2015 there were interesting
pharmaceutical products from Gilead and J & J - that tasted marketing
success:
1) Sovaldi (sofusbivir 400 mg film coated tablets),
from Gilead:
is a medication used to treat hepatitis C viral infection. This effective treatment helps reduce
peginterferon treatment (for treating hepatitis C viral infection) and also
reduces chances of liver cancer.
Sofusbivir (a nucleotide analogue drug) blocks hepatitis C virus’s DNA
polymerase enzyme thus preventing hepatitis C virus from replicating in the
body. Sovaldi sales in 2014 was 10.30 billion USD. (In the first nine months of 2014, Sovaldi
recorded sales of 8.30 billion USD).
2) Olysio
(simeprivir) and Sovriad (simeprivir) from Johnson and Johnson (Jannsen
Therapeutics division) (both are simeprivir 150 mg capsules): Olysio is an
antiviral antihepatitis C virus drug: simeprivir. It is given orally, once – a – day, in
combination with pegylated interferon and ribavirin (another antiviral drug)
for treatment of chronic HCV (Hepatitis C Virus) infection. This antiviral regimen is given to genotype 1
infected patients with chronic decompensated liver disease, including cirrhosis. Simeprivir is an oral NS3/4A protease enzyme
inhibitor (second generation protease inhibitor) (this enzyme is present in
hepatitis C virus, and inhibiting this enzyme prevents the hepatitis virus from
replicating in host cell). Olysio was launched in the end of 2013, and
in first nine months of 2014 it recorded sales 1.60 billion USD sales. Sovriad (from Jannsen) is also a brand of
simeprivir sodium 150 mg capsules and is marketed in Japan.
3)
Invokana (canagliflozin
100 mg and 300 mg film coated tablets) from Johnson and Johnson: is a
first-in-class antidiabetic drug that inhibits a protein in the kidneys called
SGLT2 (sodium glucose co-transporter 2 molecule), this protein reabsorbs the
majority of glucose filtered by kidneys.
Thus, by inhibiting SGLT2, glucose is not reabsorbed, it goes out of the
body through the urine.
4) Imbruvica
(ibrutinib 140 mg capsules) from Johnson and Johnson: is a targeted
therapy anticancer drug used for treatment of blood cancer (leukemia): where
there is increased WBC count, eg., chronic lymphocytic leukemia (this drug
attacks cancerous cells without damaging normal cells, hence, side effects are
less, ibrutinib not called a chemotherapy drug, since most chemotherapy drugs
work on the simple principle that cancer cells divide and multiply faster than
normal cells, but some normal cells also divide fast, hence, side effects with
chemotherapy drugs are more). Ibrutinib
targets an enzyme called Brutons Tyrosine Kinase (BTK). This enzyme protein molecule is required for
multiplication of malignant or cancerous WBCs (White Blood Cells). By blocking BTK, the multiplication of such
cancerous B lymphocytes (a type of WBCs) is reduced. In
2014, Imbruvica had sales of about 492 million USD.
5) Zytiga (abiraterone acetate 250 mg tablets) from
Johnson and Johnson:
This drug inhibits an enzyme called CYP17.
Zytiga is given in combination with prednisone for treatment of
resistant prostate cancer that has spread to other parts of the body. When abiraterone inhibits CYP17 (which
manifests as two enzymes), androgen synthesis is inhibited, reducing levels of
testosterone, epiandrosterone and dihydrotestosterone. By reducing blood levels of testosterone,
abiraterone helps in reducing size of prostate gland etc. 2012
sales of Zytiga was almost 1 billion USD (near block buster, at 931 million USD).
6) Invega sustenna
(paliperidone pamitate, extended release injectable suspension, for IM use;
available in 5 strengths including 39 mg, 78 mg etc.; available eg., as
pre-filled syringe of 1 ml containing equivalent to 100 mg of paliperidone)
from Johnson and Johnson: this is an atypical antipsychotic used in
schizophrenia, and as adjunct to antidepressants and mood stabilizers). This long acting injectable antipsychotic is
given once a month. In 2014, Invega sustenna generated USD 1.5 billion sales.
7) Rezolsta (fixed dose combination of darunavir 800 mg
and cobicistat 150 mg film coated tablets, pink oval shaped) from Johnson and
Johnson:
This is described as the first boosted protease inhibitor. Darunavir is a protease inhibitor (anti HIV) with good
safety and efficacy. Cobicistat is a
pharmacokinetic enhancer. This makes
darunavir easy to consume and improves patient compliance. Cobicistat and ritonavir both inhibit CYP3A4,
an enzyme. The HIV is an intracellular
parasite of the CD4 T helper lymphocytes.
The protease enzyme produced by HIV helps in replication of the HIV
inside the CD4 T helper lymphocytes (a type of WBCs). Darunavir is an enzyme that inhibits this
protease enzyme and stops the replication of HIV. Cobistat inhibits CYP3A4, an enzyme in the
liver, that breaksdown or metabolises darunavir. Hence, due to the cobistat action, darunavir
stays in the body for a longer time and is more efficacious in lowering the
viral load of HIV. Prezista (single ingredient
darunivir) had sales of 1.70
billion USD in 2013.
8) Zydelig
(idelalisib 150 mg per film coated tablet) from Gilead: this is
designated as breatkthrough designated drug launched by Gilead. This breakthrough anticancer medicine used to treat three
types of blood cancer is an oral
Phosphatidylinositol 3-kinase inhibitor.
The indications are chronic lymphocytic leukemia, follicular B cell non
Hodgkin lymphoma and small lymphocytic lymphoma.
Breakthrough designation: On July 9,
2012 the Food and Drug Administration Safety and Innovation Act (FDASIA) was
signed. FDASIA Section 902 provides for a new designation - Breakthrough
Therapy Designation.
A
breakthrough therapy is a drug:
Ø intended alone or in combination with one or more other
drugs to treat a serious or life threatening disease or condition and
Ø preliminary clinical evidence indicates that the drug may
demonstrate substantial improvement over existing therapies on one or more
clinically significant endpoints, such as substantial treatment effects observed
early in clinical development.
If a drug is designated as
breakthrough therapy, FDA will expedite the development and review of such
drug. All requests for breakthrough therapy designation will be reviewed
within 60 days of receipt, and FDA will either grant or deny the request.
Thanks for reading this rather technical blogpost on some of the fast growing and interesting
drugs of 2015. Please scroll down and read all other posts, kindly click on older posts to read other
interesting posts put up in the past: feel free to recommend this blogpost to your well-wishers.
