In March 2022, Zai Lab presented positive results from the Phase 3 PRIME study of ZEJULA (niraparib) as maintenance therapy at the Society of Gynecologic Oncology (SGO) Annual Meeting. In the PRIME study, median progression-free survival (mPFS) was significantly longer for patients treated with niraparib compared to placebo: 24.8 months versus 8.3 months, hazard ratio (HR), 0.45; p<0.001. Other pre-specified efficacy results included:

gBRCAmut patients: mPFS was not reached vs. 10.8 months; HR and 95% CI: 0.40 (0.23, 0.68).

Non-gBRCAmut patients: mPFS was 19.3 months vs. 8.3 months; HR and 95% CI: 0.48 (0.34, 0.67).

Overall survival (OS) data was still immature (percentage of death in niraparib and placebo groups are 14.5% vs. 21.7%); there was a trend in favor of niraparib at the data cut-off.

In March 2022, Zai Lab partner Novocure announced the presentation of updated results by Dr. David Tran, Chief of the Division of Neuro-Oncology at the McKnight Brain Institute at the University of Florida, from the investigator-initiated phase 2 pilot 2-THE-TOP clinical trial testing the safety and preliminary efficacy of TTFields together with pembrolizumab and temozolomide for the treatment of adult patients with newly diagnosed glioblastoma (GBM). These preliminary results, which are based on a median follow-up time on 16.8 months, compare outcomes for 26 patients in the ongoing 2-THE-TOP trial. For patients in the 2-THE-TOP trial:

mPFS was 12.1 months, compared with 7.9 months for the matched-control patients in EF-14 (hazard ratio=0.46, p=0.033).

mOS was 25.2 months, compared with 15.9 months for the matched-control patients in EF-14 (hazard ratio=0.38, p=0.020).

Of the 15 patients in 2-THE-TOP with measurable target lesions, six (40%) achieved partial to complete response and eight (53%) had stable disease.

In March 2022, Zai Lab partner Novocure announced the results of a pre-specified interim analysis for the phase 3 pivotal INNOVATE-3 study evaluating the safety and efficacy of TTFields together with paclitaxel for the treatment of patients with platinum-resistant ovarian cancer. An independent data monitoring committee (DMC) reviewed the safety data for all platinum-resistant ovarian cancer patients enrolled in the trial. The pre-specified interim analysis concluded that the INNOVATE-3 study should proceed to the final analysis as planned. Data will be reviewed in 2023, following an 18-month follow-up period.

As of March 31, 2022, Optune has been listed in 37 regional customized commercial health insurance plans guided by provincial or municipal governments (or “supplemental insurance plans”) since its commercial launch in China in the third quarter of 2020.

Topline data anticipated from the Phase 3 pivotal LUNAR clinical trial testing the efficacy of TTFields together with physician’s choice immune-checkpoint inhibitor or docetaxel for the treatment of patients with stage 4 non-small cell lung cancer (NSCLC) by year end 2022.

Last patient enrollment anticipated in the Phase 3 pivotal METIS clinical trial testing the efficacy and safety of stereotactic radiosurgery plus TTFields compared to stereotactic radiosurgery alone in patients with brain metastases resulting from NSCLC.

Report topline data from the Phase 2 pilot EF-31 clinical trial testing the safety and efficacy of TTFields together with chemotherapy in the treatment of patients with gastric cancer in 2022.

As of March 31, 2022, QINLOCK has been listed in 58 supplemental insurance plans since its commercial launch in China in May 2021.

Enroll first patients in Greater China in Mirati Therapeutics, Inc. (Mirati)’s global, potentially registrational trials in NSCLC and CRC.

Two oral presentations at the upcoming 2022 American Society of Clinical Oncology (ASCO) Annual Meeting. Presentations to include full results from the registration-enabling Phase 2 cohort of the KRYSTAL-1 study evaluating adagrasib in patients with pre-treated NSCLC harboring a KRAS^G12C mutation and late-breaking data on adagrasib in patients with KRAS^G12C-mutated NSCLC with active and untreated central nervous system metastases.

Tolerability and ORR update for the Phase 2 KRYSTAL-7 study of adagrasib in combo with pembrolizumab in first line KRAS^G12C-mutated NSCLC in the second half of 2022.

Additional clarity on the regulatory pathway of adagrasib monotherapy in first line KRAS^G12C-mutated NSCLC, and next steps for tumors other than NSCLC in the second half of 2022.

Potential FDA approval and commercial launch for adagrasib as treatment for patients with NSCLC harboring the KRAS^G12C mutation who have received at least one prior systemic therapy; PDUFA target action date of December 14, 2022.

Zai Lab partner Amgen has initiated a Phase 1b study (FORTITUDE-103) of bemarituzumab plus oral chemotherapy regimens in first line gastric cancer with FGFR2b overexpression.

Zai Lab partner Amgen is enrolling patients for a Phase 1b study (FORTITUDE-201) of bemarituzumab monotherapy and in combination with docetaxel for the treatment of squamous NSCLC with FGFR2b overexpression.

Initiate a registrational study of bemarituzumab in first-line advanced gastric and GEJ cancer in Greater China in the fourth quarter of 2022.

Planning is underway for a signal-seeking basket study in other solid tumors.

Zai Lab partner Regeneron announced that odronextamab received Fast Track designation from the FDA in follicular lymphoma (FL) and diffuse large B-cell lymphoma (DLBCL).

Complete enrollment in the potentially pivotal Phase 2 study in B-NHL.

Report additional results from the potentially pivotal Phase 2 study in B-NHL, and submit a Biologics License Application (BLA) to the FDA in the second half of 2022.

Initiate dosing with a subcutaneous formulation, the Phase 3 OLYMPIA program, and studies of additional combinations in 2022.

In April 2022, Zai Lab and Turning Point Therapeutics, Inc. (Turning Point) announced positive topline results for repotrectinib within the China region from the previously disclosed Phase 1/2 TRIDENT-1 study dataset, as reported by Blinded Independent Central Review (BICR).

In TKI-naive patients in China (EXP-1: n=11), the confirmed objective response rate (cORR) was 91% (95% CI: 59,100).

In TKI-pretreated patients in China, the cORR was 67% in those treated with 1 TKI and platinum-based chemotherapy (EXP-2: n=3); the cORR was 50% in those treated with two TKIs globally (EXP-3: n=4); the cORR was 36% in those treated with 1 TKI (EXP-4: n=11).

In April 2022, Zai Lab partner Turning Point announced positive topline results from the registrational TRIDENT-1 study across all four ROS1-positive advanced NSCLC cohorts, as reported by BICR.

In TKI-naïve patients (EXP-1: n=71), the cORR was 79% (95% CI: 68, 88).

In TKI-pretreated patients, the cORR was 42% in those treated with 1 TKI and platinum-based chemotherapy (EXP-2: n=26); the cORR was 28% in those treated with two TKIs (EXP-3: n=18); the cORR was 36% in those treated with 1 TKI (EXP-4: n=56).

In TKI-pretreated patients with an identified ROS1 G2032R solvent front mutation, the cORR was 59% (n=10/17; 95% CI: 33, 82).

In March 2022, Zai Lab partner Turning Point announced that the company has achieved its enrollment target of 40 patients in the EXP-6 cohort of the phase 1/2 registrational TRIDENT-1 study. EXP-6 is comprised of NTRK-positive TKI-pretreated advanced solid tumor patients.

Complete enrollment in the phase 1/2 registrational TRIDENT-1 study.

Discuss the regulatory pathway with the National Medical Products Administration (NMPA) at a pre-NDA meeting in the fourth quarter of 2022.

Discuss the topline BICR data with the FDA at a pre-NDA meeting in the second quarter of 2022.

Anticipate providing a detailed update from TRIDENT-1 utilizing BICR analyses, including intracranial activity, at an upcoming medical conference in the second half of 2022.

Provide a clinical data update from the NTRK-positive advanced solid tumor cohorts from TRIDENT-1 in the second half of 2022.

In March 2022, Zai Lab partner Cullinan Oncology announced the clinical and regulatory updates for CLN-081 in NSCLC EGFR exon 20 patients. Key highlights of 100mg BID dose level in the ongoing Phase 1/2a study:

Of 39 response evaluable patients, 16 achieved a confirmed partial response for a 41% cORR.

No patients have experienced Grade 3 or greater treatment-related diarrhea or rash.

Promising response durability previously observed in initial phase 1 patient cohort (n=13) with estimated median response duration > 15 months and mPFS of 12 months.

Enroll the first patient in Greater China in the Phase 2a potentially pivotal study in NSCLC.

Updated CLN-081 data accepted for oral presentation at the ASCO 2022 Annual Meeting.

Initiate a pivotal study in the second half of 2022 following the completion of a pharmacokinetic (PK) food effect study.

Enroll the first patient in Greater China in the Phase 1 expansion portion of the global Phase 1/2 SHIELD-1 study.

Provide a clinical data update from the Phase 1 SHIELD-1 study in the second half of 2022.

Initiate the Phase 2 portion of the SHIELD-1 study in the second half of 2022, pending FDA feedback on data from the intermediate dose level.

Initiate the Phase 1b/2 SHIELD-2 combination study of elzovantinib and aumolertinib in mid-2022.

As previously disclosed and based on a review of the clinical data and the changing treatment landscape, we have decided to complete and close trial enrollment for the study of retifanlimab in MSI-H/dMMR endometrial cancer in Greater China.

Complete enrollment in the global Phase 3 POD1UM-304 study evaluating retifanlimab in combination with platinum-based chemotherapy in patients with first-line metastatic NSCLC.

In April 2022, Zai Lab’s partner Blueprint Medicines Corporation announced the proof-of-concept data from the Phase 1/2 SYMPHONY clinical trial of BLU-945 in advanced EGFR-driven NSCLC patients at the 2022 American Association for Cancer Research (AACR) Annual Meeting. The preliminary trial results showed early evidence of safety and clinical activity consistent with preclinical data, supporting plans to expand development of BLU-945 in combination with multiple agents including osimertinib.

Blueprint Medicines is initiating a cohort in the ongoing Phase 1/2 SYMPHONY trial assessing BLU-945 in combination with osimertinib in patients with second-line or later EGFR-mutant NSCLC.

Present initial clinical data from the dose escalation cohort of the Phase 1/2 SYMPHONY trial evaluating BLU-945 in combination with osimertinib in the second half of 2022.

Initiate additional cohorts in the Phase 1/2 SYMPHONY trial for BLU-945 in combination with other agents across multiple patient populations, including early line therapy.

Zai Lab’s partner Blueprint Medicines presented preclinical data at the AACR Annual Meeting in April 2022 demonstrating potent antitumor activity of BLU-945 and BLU-701 on models of L858R-driven disease, with or without on-target resistance, supporting the development of both investigational agents in combination in the first- and second-line EGFR-driven NSCLC settings.

Present initial Phase 1/2 HARMONY trial data for BLU-701 in EGFR-driven NSCLC in the second half of 2022.

In April 2022, Zai Lab presented new data from the internal oncology discovery portfolio at the 2022 AACR Annual Meeting.

First preview of preclinical data for ZL-1218, an anti-CCR8 antibody, in an oral presentation.

Poster presentations featured ZL-1201 (anti-CD47 antibody) for advanced hematologic malignancies and solid tumors, ZL-1211 (anti-CLDN18.2 antibody) for gastric and pancreatic cancer and ZL-2201 (DNA-PK inhibitor) for solid tumors.

Initiate a Phase 2 proof-of-concept study in the second quarter of 2022.

Determine a recommended Phase 2 dose in the ongoing Phase 1 trial in mid-2022.

In May 2022, Zai Lab partner argenx announced positive topline data from the Phase 3 ADVANCE trial of efgartigimod for the treatment of primary immune thrombocytopenia (ITP). ADVANCE met its primary endpoint demonstrating a significantly higher proportion of patients with chronic ITP receiving efgartigimod (17/78; 21.8%) compared to placebo (2/40; 5%) achieved a sustained platelet response (p=0.0316). Key platelet-derived secondary endpoints also demonstrated statistical significance.

In April 2022, Zai Lab partner argenx announced interim results from the ongoing Phase 3 ADAPT+ study, an open-label, extension study evaluating the long-term efficacy, safety, and tolerability of efgartigimod for the treatment of adults with generalized myasthenia gravis (gMG). Interim data suggest that efgartigimod provides consistent improvement over multiple treatment cycles with a safety profile as seen in the Phase 3 ADAPT study.

In March 2022, Zai Lab partner argenx announced positive topline data from the Phase 3 ADAPT-SC study evaluating subcutaneous (SC) efgartigimod for the treatment of gMG. SC efgartigimod achieved the primary endpoint of total IgG reduction from baseline at Day 29, demonstrating statistical noninferiority to the intravenous (IV) formulation of efgartigimod in gMG patients.

Submit the NDA to the NMPA for gMG in mid-2022.

Launch proof-of-concept trials in two autoimmune renal diseases in 2022.

Continue to explore and advance additional indications in coordination with argenx.

Initiate the registrational ALKIVIA trial in the second quarter of 2022 for three subtypes of idiopathic inflammatory myopathies (myositis), including immune-mediated necrotizing myopathy, anti-synthetase syndrome and dermatomyositis; interim analysis planned of first 30 patients of each subtype.

Submit a BLA to the FDA for SC efgartigimod in gMG by the end of 2022.

Initiate a global Phase 2 study for CPP in the second half of 2022.

Seek National Reimbursement Drug List (NRDL) inclusion for CABP and ABSSSI indications.

Submit Zai Lab’s plan for post-approval studies in the second half of 2022.

In April 2022, Zai Lab partner Entasis Therapeutics presented top-line data from the pivotal Phase 3 ATTACK trial at the 32nd European Congress of Clinical Microbiology and Infectious Diseases (ECCMID) Annual Conference in Lisbon.

Submit an NDA to the NMPA in the fourth quarter of 2022.

Submit an NDA to the FDA in mid-2022.

Seek regulatory agreement with the NMPA on a China program in schizophrenia in mid-2022.

Initiate the bridging study program.

The Phase 3 EMERGENT-2 trial completed enrollment in the second quarter of 2022. Topline data from the trial anticipated in the third quarter of 2022.

Initiate Phase 3 program evaluating KarXT as a treatment for psychosis in Alzheimer’s disease in mid-2022. Details of the program to be shared in the first half of 2022.

In April 2022, Zai Lab announced that the Audit Committee of its Board of Directors has approved the engagement of KPMG LLP (KPMG) as Zai Lab’s independent registered public accounting firm. KPMG will be engaged to audit the annual consolidated financial statements of Zai Lab and its subsidiaries filed with the U.S. Securities and Exchange Commission and our internal controls over financial reporting for the fiscal year ending December 31, 2022. Zai Lab expects that this transition to an audit firm located in the United States and subject to inspection by the Public Company Accounting Oversight Board (PCAOB) enables Zai Lab to comply with the audit requirements of the Holding Foreign Companies Accountable Act and, if so, will facilitate its continued listing on Nasdaq.

In March 2022, the shareholders of Zai Lab approved a one-to-ten share subdivision, effective March 30, 2022. The one-to-ten share subdivision will increase the number of ordinary shares of Zai Lab in issue and reduce the nominal value and trading price of each ordinary share. The Board of Directors of the Company believes that this will increase the trading liquidity of the ordinary shares, lower the investment barrier, and will attract more investors to trade in the ordinary shares. The share subdivision did not result in any change to the number of outstanding American Depositary Shares (ADSs) of the Company.

Zai Lab continues to strengthen and expand its global leadership team. In March 2022, Zai Lab announced the appointment of Josh Smiley as its Chief Operating Officer (COO), effective in August 2022. Mr. Smiley brings over 26 years of experience working within the biopharmaceutical industry, including experience leading finance, corporate strategy, business development, venture capital, and the Global Business Services operations at Eli Lilly and Co (Lilly).

As of March 31, 2022, Zai Lab employed 1,999 full-time employees, including 825 and 950 employees engaged in R&D and commercial activities, respectively.

For the three months ended March 31, 2022, total revenues were $46.7 million, compared to $20.1 million for the same period in 2021. Product revenues for the period were $29.6 million for ZEJULA, compared to $12.6 million for the same period in 2021; $12.8 million for Optune, compared to $7.1 million for the same period in 2021; $3.0 million for QINLOCK, compared to $0.4 million for the same period in 2021, and $0.7 million for NUZYRA, compared to nil for the same period in 2021.

Research and Development (R&D) expenses were $53.9 million for the three months ended March 31, 2022, compared to $203.9 million for the same period in 2021. The decrease in R&D expenses was primarily due to no upfront payment for new licensing agreements, partially offset by increased expenses related to ongoing and newly initiated late-stage clinical trials and higher payroll and payroll-related expenses from increased R&D headcount. Excluding upfront payment for new licensing agreements, core R&D expenses were $53.9 million for the three months ended March 31, 2022, compared to $41.6 million for the same period in 2021.

Selling, General and Administrative (SG&A) expenses were $57.0 million for the three months ended March 31, 2022, compared to $35.8 million for the same period in 2021. The increase was primarily due to payroll and payroll-related expenses from increased commercial and general and administrative headcount, as Zai Lab continued to expand and invest in its commercial operations in China in anticipation of substantial topline growth over the next few years.

Net Loss was $82.4 million for the three months ended March 31, 2022 compared to $232.9 million for the same period in 2021, primarily due to no upfront payment for new licensing agreements. Net loss per ordinary share during the three months ended March 31, 2022 was $0.09, compared to $0.26 for the same period in 2021. Net loss per ADS during the three months ended March 31, 2022 was $0.86, compared to $2.64 for the same period in 2021.

As of March 31, 2022, cash and cash equivalents, short-term investments and restricted cash totaled $1,313.0 million compared to $1,409.9 million as of December 31, 2021.

Assets

Current assets:

Cash and cash equivalents

Short-term investments

Accounts receivable (net of allowance for credit loss of $10 and $11 as of March 31, 2022 and December 31, 2021, respectively)

Notes receivable

Inventories

Prepayments and other current assets

Total current assets

Restricted cash, non-current

Long term investments (including the fair value measured investment of $8,444 and $15,383 as of March 31, 2022 and December 31, 2021, respectively)

Prepayments for equipment

Property and equipment, net

Operating lease right-of-use assets

Land use rights, net

Intangible assets, net

Long-term deposits

Value added tax recoverable

Total assets

Liabilities and shareholders’ equity

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Accounts payable

Current operating lease liabilities

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Total current liabilities

Deferred income

Non-current operating lease liabilities

Total liabilities

Shareholders’ equity

Ordinary shares (par value of $0.000006 per share; 5,000,000,000 shares authorized; 957,035,440 and 955,363,980 shares issued as of March 31, 2022 and December 31, 2021, respectively; 956,637,360 and 954,981,050 shares outstanding as of March 31, 2022 and December 31, 2021, respectively)

Additional paid-in capital

Accumulated deficit

Accumulated other comprehensive loss

Treasury Stock (at cost, 398,080 and 382,930 shares as of March 31, 2022 and December 31, 2021, respectively)

Total shareholders’ equity

Total liabilities and shareholders’ equity

Revenues:

Product revenue, net

Collaboration revenue

Total revenues

Expenses:

Cost of sales

Research and development

Selling, general and administrative

Loss from operations

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Other expenses, net

Loss before income tax and share of loss from equity method investment

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Net loss

Net loss attributable to ordinary shareholders

Loss per share - basic and diluted

Weighted-average shares used in calculating net loss per ordinary share - basic and diluted (Note)

Loss per American Depositary Shares (“ADS”) (Note) - basic and diluted

Weighted-average ADS used in calculating net loss per ADS - basic and diluted

Net loss

Other comprehensive (loss) income, net of tax of nil:

Foreign currency translation adjustments

Comprehensive loss