Zentalis Steps Out With $147M Raised to Develop “Tried and True” Small Molecules

Zentalis Pharmaceuticals is banking on small molecules for cancer—leaving the “cool technologies” aside for a “tried and true” approach, says the CEO, who wants to let the science speak for itself.

Since it was founded five years ago, the company has moved three compounds into the clinic. How? By operating under the radar. “If you take away the outside distractions, which is what we’ve been doing; when you have that singular focus, which is to develop drugs, it really helps,” Zentalis Pharmaceuticals CEO Anthony Sun tells Xconomy.

The company this week emerged from “stealth mode” after closing an $85 million (€77 million) Series C financing round—bringing its total funds raised since 2014 to $147 million.

Proceeds from the round will be used to advance the company’s clinical pipeline of potentially best-in-class novel small molecule therapeutics.

“We’ve been making small molecules for decades. We know how they work, we know how to make them at metric ton levels. We forget these things as the cool science outweighs the tried and true, which is small molecules,” says Sun, speaking to the advantages of the company’s approach.

“We are all enamored by cool technologies, but if you can really build a platform of small molecule oncology, go after fundamental cancer pathways, this is something that could really reap benefits for patients,” he adds. “This is why we’ve decided to go after this field in this fashion.”

The company currently has three internally developed programs in the clinic—soon to be four.

Among these is the company’s lead product candidate, ZN-c5, an oral Selective Estrogen Receptor Degrader (SERD) for estrogen receptor-positive, HER2-negative (ER+/ HER2-) breast cancer. The experimental treatment is being developed as a monotherapy and in combination with Ibrance (palbociclib), Pfizer’s CDK4/6 inhibitor approved for ER+/HER2- advanced breast cancer patients in combination with hormonal therapies. The companies have been working together since May 2018.

Zentalis also is working with SciClone Pharmaceuticals to develop a potential treatment for lung cancer. As per the company’s collaboration strategy, Sun says it’s “about what the science tells us to do.”

“If the science says our drug works best with Pfizer’s drug—let’s go test it out. If it’s best to be used in monotherapy, that’s what we’ll do,” he says. “We don’t let the partnership decide what to do, we let the science speak for itself.”

The company—also targeting solid tumors and hematologic cancer—currently has 60 employees, though Sun says this number will likely be closer to 100 next year.

As part of this growth, the company also is moving into larger lab space in the Torrey Pines area of San Diego during the second half of 2020. “It’s a great place to recruit scientists,” says Sun, speaking to the company’s location. “There’s a vibrant community there, so we’ve capitalized on that.”

The corporate headquarters are in Manhattan where most of the C-suites reside.

Zentalis’ Series A round in 2015 was led by Viking Global, Mayo Clinic, Alexandria, and Pharmaron. Two years later, Matrix Capital, Perceptive Advisors, and Highlight Capital joined the institutional investors for the Series B.

New investors participating in this Series C financing include Eventide Asset Management, Redmile Group, and Surveyor Capital (a Citadel company). Matrix Capital, Viking Global Investors, Farallon Capital, and Perceptive Advisors also returned for the financing.

(Image: iStock/AlexRaths)