|ACT-GRO-777 (DNA aptamer)
In April 2011, ACT acquired 100% rights to Antisoma’s clinical
stage asset, AS1411, now referred to as ACT-GRO-777. ACT-GRO-777 is
an aptamer that binds to a protein called nucleolin which is found on
the surface of many cancer cells. ACT-GRO-777 binds to nucleolin and
causes cancer cell death. Phase I and II human clinical trials have
reported evidence of anti-cancer activity and a favorable safety profile.
ACT is evaluating ACT-GRO-777 for additional human cancer trials in
collaboration with the James Graham Brown Cancer Center.
PU27 (Oligo Quadruplex)
PU27 is a synthetic oligonucleotide
which is a novel anticancer compound. It represents a
naturally occurring, genomic DNA sequence which is present
in two copies in every human cell. PU27 has
the ability to form four-stranded (quadruplex) DNA and
is located in the promoter of the c-myc gene, a gene
which is involved in more than 80% of human tumors. We
have demonstrated that the addition of exogenous PU27 inhibits
the growth of cancer cells but has no effect on nonmalignant
PU27 is active against a wide
variety of tumor types, including leukemia, prostate
cancer, renal cancer and
breast cancer cell lines. The growth inhibitory activity
of PU27 was discovered because
of its ability to bind and inhibit the enzymatic activity
of a-enolase, a glycolytic
pathway enzyme. Treated cells also demonstrate altered
oncogene expression and decreased telomerase activity.
The ability of PU27 to selectively inhibit cancer cell
metabolism and cell growth has important implications
for its use as an anticancer agent.
PFKFB3 (small molecule)
High glucose consumption is common in cancer cells versus normal cells.
3PO is a novel small molecule which has already demonstrated anti-cancer
effects in five (5) different animal cancer models. Involving both hematological
(blood cancers) and solid tumors, there have been no noticeable toxic
affects to these animals at low and high doses. 3PO's novel mechanism
of action blocks the uptake of glucose in cancer cells, starving cancer
cells of an important source of energy needed for growth and disease
progression. Based on our in-depth knowledge of this key molecular target
in oncology, ACT is developing a series of next generation small molecule
compounds through its medicinal chemistry efforts.
Choline Kinase (small molecule)
Choline metabolism is altered in a wide variety of cancers including,
lung, breast, ovarian, brain, and prostate cancers. Choline Kinase,
the enzyme responsible for the generation of phosphocholine, is the
most important enzyme associated with choline metabolism and cell proliferation
and is over expressed in most solid tumors. A small molecule, referred
to as CK37, inhibits cell proliferation, choline kinase enzymatic activity,
and tumor growth in xenograft studies without signs of toxicity. ACT’s
medicinal chemistry group is developing analogs to optimize the biologic
and pharmacologic properties of CK37 prior to initiating IND enabling
Human Papillomavirus (HPV) is a leading cause of cervical cancer and approximately
20 million people are currently infected with this sexually transmitted disease
(STD). According to the Centers For Disease Control and Prevention, at least
80 percent of women will have acquired genital HPV infection by age 50 with
about 6.2 million Americans contracting a new genital HPV infection each year.
The U.S. FDA recently approved the first HPV cervical cancer vaccine that includes
a portion of the L1 capsid protein (Gardasil by Merck & Co.) to guard against
this terrible disease. Advanced Cancer Therapeutics is developing a novel HPV
vaccine which targets the L2 capsid protein that we believe should provide
broader immune protection to patients at risk of contracting cervical cancer.
ACT intends to manufacture its novel HPV vaccine from tobacco mosaic plants,
promising to be very cost effective for people at risk of contracting HPV in
both developed and developing nations